[ CAS No. 6281-42-1 ] {[proInfo.proName]}

Name: 6281-42-1|1-(2-Aminoethyl)imidazolidin-2-one|97%
Brand: Ambeed
SKU: A139435
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Quality Control of [ 6281-42-1 ]

COA NMR CNMR HPLC LC-MS

Related Doc. of [ 6281-42-1 ]

SDS Specification

Alternatived Products of [ 6281-42-1 ]

Product Details of [ 6281-42-1 ]

CAS No. :	6281-42-1	MDL No. :	MFCD00086348
Formula :	C₅H₁₁N₃O	Boiling Point :	-
Linear Structure Formula :	-	InChI Key :	PODSUMUEKRUDEI-UHFFFAOYSA-N
M.W :	129.16	Pubchem ID :	80480
Synonyms :

Calculated chemistry of [ 6281-42-1 ]

Physicochemical Properties

Num. heavy atoms :	9
Num. arom. heavy atoms :	0
Fraction Csp3 :	0.8
Num. rotatable bonds :	2
Num. H-bond acceptors :	2.0
Num. H-bond donors :	2.0
Molar Refractivity :	40.86
TPSA :	58.36 Å²

Pharmacokinetics

GI absorption :	Low
BBB permeant :	No
P-gp substrate :	No
CYP1A2 inhibitor :	No
CYP2C19 inhibitor :	No
CYP2C9 inhibitor :	No
CYP2D6 inhibitor :	No
CYP3A4 inhibitor :	No
Log Kp (skin permeation) :	-8.23 cm/s

Lipophilicity

Log Po/w (iLOGP) :	0.88
Log Po/w (XLOGP3) :	-1.61
Log Po/w (WLOGP) :	-1.79
Log Po/w (MLOGP) :	-0.82
Log Po/w (SILICOS-IT) :	-0.59
Consensus Log Po/w :	-0.79

Druglikeness

Lipinski :	0.0
Ghose :	None
Veber :	0.0
Egan :	0.0
Muegge :	1.0
Bioavailability Score :	0.55

Water Solubility

Log S (ESOL) :	0.51
Solubility :	414.0 mg/ml ; 3.2 mol/l
Class :	Highly soluble
Log S (Ali) :	0.89
Solubility :	1010.0 mg/ml ; 7.83 mol/l
Class :	Highly soluble
Log S (SILICOS-IT) :	-0.4
Solubility :	51.5 mg/ml ; 0.399 mol/l
Class :	Soluble

Medicinal Chemistry

PAINS :	0.0 alert
Brenk :	0.0 alert
Leadlikeness :	1.0
Synthetic accessibility :	1.77

Safety of [ 6281-42-1 ]

Signal Word:	Danger	Class:	8
Precautionary Statements:	P280-P305+P351+P338-P310	UN#:	3259
Hazard Statements:	H314	Packing Group:	Ⅲ
GHS Pictogram:

Application In Synthesis of [ 6281-42-1 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

Upstream synthesis route of [ 6281-42-1 ]
Downstream synthetic route of [ 6281-42-1 ]

[ 6281-42-1 ] Synthesis Path-Upstream 1~9

1
[ 111-40-0 ]
[ 57-13-6 ]
[ 6281-42-1 ]

Yield	Reaction Conditions	Operation in experiment
96%	at 125 - 160℃; Inert atmosphere; Large scale	693 kg (6728 M) of DETA were introduced into a 1 m³stirred reactor which has a double jacket, a device for introducing liquid, a nitrogen inerting system, a container and a scrubbing column for recovering the ammonia gas and the aqueous ammoniacal liquors. The reaction medium was brought to 130° C. while at the same time performing nitrogen sparging so as to deoxygenate the DETA. When the temperature was reached, the introduction of an aqueous solution of urea at 40percent, on the basis of 671.4 kg (4476 M), was begun. The DETA:urea molar ratio was therefore 1.5:1.[0045]The urea was introduced fractionwise over the course of 4 h.[0046]The release of ammonia, which appeared at soon as the running-in began, was scrubbed on the scrubbing column and the aqueous ammoniacal liquors were collected in the container. The reaction mixture was then kept at 130° C. for 1 h30 in order to finish off the removal of the water.[0047]The reaction medium was then gradually heated by bringing it: to 140° C. for 45 min, then to 150° C. for 45 min, then to 160° C. for 5 h. It was cooled to 125° C. at the end of the reaction, and then the excess DETA was removed under reduced pressure of from 10 to 1.5 mbar and with mild nitrogen sparging, for a maximum of 5 h. The product obtained after returning the equipment to atmospheric pressure, cooling to 60° C. and withdrawal from the reactor had a UDETA titer of 95-96percent and contained 1-2.5percent of TETU

Reference： [1] Patent: US2013/23667, 2013, A1, . Location in patent: Paragraph 0044; 0045; 0046; 0047
[2] Patent: US2613212, 1950, ,
[3] Patent: US6630599, 2003, B1, . Location in patent: Page/Page column 10

2
[ 111-40-0 ]
[ 616-38-6 ]
[ 6281-42-1 ]

Reference： [1] Patent: EP2548869, 2013, A1, . Location in patent: Paragraph 0041; 0042
[2] Patent: WO2013/12995, 2013, A1, . Location in patent: Page/Page column 18

3
[ 111-40-0 ]
[ 6281-42-1 ]

Reference： [1] Patent: EP928820, 1999, A2,
[2] Patent: EP810996, 2002, B1,

4
[ 757967-03-6 ]
[ 103-82-2 ]
[ 6281-42-1 ]
[ 100-02-7 ]
[ 623-05-2 ]
[ 124-38-9 ]

Reference： [1] Patent: US2006/269480, 2006, A1, . Location in patent: Page/Page column 24; sheet 2; 3

5
[ 2387-20-4 ]
[ 6281-42-1 ]

Reference： [1] Journal of the American Chemical Society, 1957, vol. 79, p. 5276,5279

6
[ 124-38-9 ]
[ 111-40-0 ]
[ 6281-42-1 ]

Reference： [1] ChemCatChem, 2013, vol. 5, # 4, p. 1020 - 1023

7
[ 40778-59-4 ]
[ 6281-42-1 ]

Reference： [1] Journal of the American Chemical Society, 1956, vol. 78, p. 6144[2] Journal of the American Chemical Society, 1957, vol. 79, p. 5276,5278
[3] Canadian Journal of Chemistry, 1957, vol. 35, p. 843,848

8
[ 6573-15-5 ]
[ 6281-42-1 ]

Reference： [1] Canadian Journal of Chemistry, 1957, vol. 35, p. 843,848

9
[ 2387-20-4 ]
[ 98137-74-7 ]
[ 6281-42-1 ]

Reference： [1] Journal of the American Chemical Society, 1957, vol. 79, p. 5276,5279

[ 6281-42-1 ] Synthesis Path-Downstream 1~88

1
[ 77-77-0 ]
[ 6281-42-1 ]
[ 85694-70-8 ]

Reference： [1]Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry,1982,vol. 21,p. 928 - 940

2
[ 6281-42-1 ]
[ 93849-15-1 ]
[ 123700-21-0 ]

Reference： [1]Journal of Medicinal Chemistry,1990,vol. 33,p. 585 - 591

3
[ 753482-69-8 ]
[ 6281-42-1 ]
4-methyl-8-(morpholine-4-sulfonyl)-2-[2-(2-oxo-imidazolidin-1-yl)-ethyl]-pyrrolo[3,4-<i>c</i>]quinoline-1,3-dione [ No CAS ]

Reference： [1]European Journal of Medicinal Chemistry,2005,vol. 40,p. 1377 - 1383

4
[ 6281-42-1 ]
[ 1007554-45-1 ]
1-(2-(6-phenyl-5-(pyridin-4-yl)pyridazin-3-ylamino)ethyl)imidazolidin-2-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	In butan-1-ol; at 130℃; for 24h;	Compound 6 is aminated using 6 equiv of 1-(2-aminoethyl)imidazolidin-2-one in 1-butanol at 130 C. in a pressure vessel for 24 hrs, the mixture concentrated under reduced pressure, ethylacetate added and washed with water, then dried over anhydrous sodium sulphate. The crude product is purified by recrystallization in methanol/hexane. Purity >98%, ESI m/z 361.63, (MH+), M.P. 205.5-206.7 C. (uncorrected).

Reference： [1]Patent: US2008/51410,2008,A1 .Location in patent: Page/Page column 15; sheet 1

5
[ 6281-42-1 ]
[ 50329-91-4 ]
C₁₅H₁₅N₃O₄ [ No CAS ]

Reference： [1]Chemistry of Heterocyclic Compounds,2006,vol. 42,p. 574 - 582

6
[ 6281-42-1 ]
[ 4971-43-1 ]

Reference： [1]Patent: US2787619,1955,

7
[ 6281-42-1 ]
[ 86024-61-5 ]

Reference： [1]Patent: US2881171,1955,

8
[ 4427-96-7 ]
[ 6281-42-1 ]
C₁₀H₁₇N₃O₄ [ No CAS ]
C₁₀H₁₇N₃O₄ [ No CAS ]

Reference： [1]Patent: EP1167356,2002,A2 .Location in patent: Page 6

9
4-formyl-3-methoxyphenoxy resin [ No CAS ]
[ 6281-42-1 ]
AG-MB-1-(2-aminoethyl)-imidazolidin-2-one [ No CAS ]

Reference： [1]Patent: US6359061,2002,B1 .Location in patent: Example 1

10
[ 6281-42-1 ]
[ 660870-46-2 ]
methyl 5-[5-([2-(2-oxoimidazolidin-1-yl)ethyl]amino}carbonyl)-1H-benzimidazol-1-yl]-3-[2-(trifluoromethyl)benzyl]oxy}thiophene-2-carboxylate [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
95%	With N-ethyl-N,N-diisopropylamine; HATU; In DMF (N,N-dimethyl-formamide); for 2h;	To a solution of [1-(5-(METHOXYEARBONYL)-4-[2-(TRIFLUOROMETHYL) BENZYL] OXY}] thien-2- yl)-1 H-benzimidazole-5-carboxylic acid (112 mg, 0.23 [MMOL),] [1- (2-] aminoethyl) imidazolidin-2-one (85 mg, 0.35 mmol) and diisopropylethylamine (110 [MICROL,] 0.62 mmol) in dimethylformamide (2.0 mL) was added [[0- (7-AZABENZOTRIAZOL-] 1-yl)-1, 1,3, 3-tetramethyluronium hezafluorophosphate] (115 mg, 0.30 [MMOL).] The reaction was stirred for 2 hours then poured into ethyl acetate and washed with aqueous 5% HCI, aqueous saturated [NAHCO3,] water, brine, and dried over Na2SO4. Filtration and concentration gave crude methyl 5-[5-([2-(2-oxoimidazolidin-1- yl) ethyl]amino}carbonyl)-1H-benzimidazol-1-yl]-3-[2-(trifluoromethyl)- benzyl] oxy} thiophene-2-carboxylate (128 mg, 95%) as tan solid. The solid was stirred as a solution in 7 M ammonia in methanol (10 mL, 70 [MMOL),] at [80C] in a sealed, thick-walled glass pressure tube for 16 hours. The reaction was cooled to -10C and cold diethyl ether was added. The resulting slurry was filtered, washing the solids with cold diethyl ether. The solids were then dried under vacuum to give [1- (5-] (aminocarbonyl)-4- { [[2-] [UOROMETHYL) BENZYL] OXY} TH IEN-2-YL)-N-[2-(2-] [OXOIMIDAZOLIDIN-1-YL) ETHYL]-1 H-BENZIMIDAZOLE-5-CARBOXAMIDE] (53 mg, 44%) as a white [SOLID.'H] NMR (400 MHz, [DMSO-D6)] [8] 8.75 (s, 1 H), 8.64 (t, [J =] 5.49 Hz, [1H),] 8.28 (s, [1 H),] 7.70-7. 94 (m, [7H),] 7.65 (t, J = 7.60 Hz, [1 H),] 6.79 (b, [1 H),] 6.28 (s, 1 H), 5.55 (s, 2H), 3.36-3. 44 (m, 4H), 3.18-3. 27 (m, 4H). MS [(ES+,] [M/Z)] 572 [(M+1).]

Reference： [1]Patent: WO2004/14899,2004,A1 .Location in patent: Page 190-191

11
[ 6281-42-1 ]
[ 82417-45-6 ]
[ 886236-60-8 ]

Yield	Reaction Conditions	Operation in experiment
87%	With triethylamine; In tetrahydrofuran; at 20℃;	17a) 2,3-Dichloro-N-[2-(2-oxoimidazolidin-1-yl)ethyl]benzenesulphonamide A solution of 0.5 g (2.04 mmol) of 2,3-dichlorobenzenesulphonyl chloride, 0.26 g (2.04 mmol) of 1-(2-aminoethyl)-2-imidazolidone and 1 ml (7.18 mmol) of triethylamine in 10 ml of tetrahydrofuran was stirred at room temperature overnight. The reaction mixture was then washed with 1 N HCl and saturated sodium bicarbonate solution, dried over sodium sulphate and concentrated. The product obtained in this manner was reacted further without additional purification. C11H13Cl2N3O3S (338.21) Yield: 87% of theory 1H-NMR (d6-DMSO): delta=2.99 (m, 2H), 3.07 (m, 2H), 3.15 (m, 2H), 3.27 (m, 2H), 6.27 (s br, NH), 7.56 (t, 1H), 7.92 (d, 1H), 7.96 (d, 1H), 8.13 (t br, NH) ppm

Reference： [1]Patent: US2006/100219,2006,A1 .Location in patent: Page/Page column 22

12
[ 6281-42-1 ]
[ 893434-89-4 ]
1-(2-(4-(benzo[b]thiophen-2-yl)pyrimidin-2-ylamino)ethyl)imidazolidin-2-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
64%	With triethylamine; In 2-methoxy-ethanol; at 100℃;	A mixture of 4-(benzo[b]thiophen-2-yl)-2-(methylsulfonyl)pyrimidine (75 mg, 0.26 mmol)), l-(2-aminoethyl)imidazolidin-2-one (33 mg, 0.26 mmol) and triethylamine (32mg, 0.31 mmol) in methoxyethanol (3 mL) was heated at 100 C overnight. After cooling to rt the solvent was removed in vacuo and the product was purified by chromatography eluting with methanol / dichloromethane (1:20) to give the title compound as a slightly yellow solid (56 mg, 64%). MS (M+H)+ 340.

Reference： [1]Patent: WO2006/66172,2006,A1 .Location in patent: Page/Page column 39

13
[ 6281-42-1 ]
[ 893441-65-1 ]
1-(2-(4-(5-(morpholinosulfonyl)thiophen-2-yl)pyrimidin-2-ylamino)ethyl)imidazolidin-2-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
72%	With triethylamine; In toluene; for 6h;Heating / reflux;	A mixture of 2-(meylsulfonyl)-4-(5-(mophiholinosulfonyl)thiophen-2-yl)pyrimidine (100 mg, 0.26 mmol), l-(2-aminoethyl)imidazolidin-2-one (36 mg, 0.28 mmol) and triethylamine (56 mg, 0.52 mmol) in toluene (3 mL) was refluxed for 6 h. After cooling to rt, the solvent was evaporated in vacuo and then methanol (5 mL) was added. After stirring for 15 min the solid was filtered and dried to give the title compound with a light yellow color (81 mg, 72%). MS (M+H)+ 439.

Reference： [1]Patent: WO2006/66172,2006,A1 .Location in patent: Page/Page column 54

14
[ 6281-42-1 ]
[ 893441-68-4 ]
1-(2-(4-(5-(morpholine-4-carbonyl)thiophen-2-yl)pyrimidin-2-ylamino)ethyl)-imidazolidin-2-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	With triethylamine; In toluene; for 6h;Heating / reflux;	A mixture of (5-(2-(methylsulfonyl)pyrimidin-4-yl)thiophen-2-yl)(morpholino)methanone(100 mg, 0.26 mmol), l-(2-aminoethyl)imidazolidin-2-one (36 mg, 0.28 mmol) and triethylamine (56 mg, 0.52 mmol) in toluene (3 mL) was refluxed for 6 h. After cooling to it, the solvent was evaporated in vacuo and then methanol (5 mL) was added. After stirring for 15 min the solid was filtered and dried to give title compound as a light yellow solid. MS (M+H)+ 403.

Reference： [1]Patent: WO2006/66172,2006,A1 .Location in patent: Page/Page column 59

15
[ 6281-42-1 ]
[ 131022-68-9 ]
1-(2-(4-(5-bromothiophen-2-yl)pyrimidin-2-ylamino)ethyl)imidazolidin-2-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
68%	With triethylamine; In isopropyl alcohol; for 30h;Heating / reflux;	A mixture of 4-(5-bromothiophen-2-yl)-2-chloropyrimidine (1.0 g, 3.63 mmol), l-(2- aminoethyl)imidazolidin-2-one (0.47 g, 3.63 mmol) and triethylame (0.44 g, 4.36 mmol) in isopropanol (25 mL) was refluxed for 30 h. After cooling down to rt the precipitate was filtered and washed with methanol (5 mL) and dried to give the title compound as a yellow solid (0.9 g, 68%). MS (M+H)+ 368/370.

Reference： [1]Patent: WO2006/66172,2006,A1 .Location in patent: Page/Page column 31

Yield	Reaction Conditions	Operation in experiment
44%		EXAMPLE 8 2-{2-Ethoxy-5-[2-(1-imidazolidin-2-onyl)ethyl-sulphamoyl)-phenyl}-8-n-propylpyrido[3,2-d]pyrimidin-4-(3H)-one Obtained using 1-(2-aminoethyl)imidazolidin-2-one in 44% yield, m.p. 221-222 C.

Yield	Reaction Conditions	Operation in experiment
44%		EXAMPLE 8 2-{2-Ethoxy-5-[2-(1-imidazolidin-2-onyl)ethyl-sulphamoyl]phenyl}-8-n-propylprido[3,2-d]pryimidin-4 (3H)-one Obtained using 1-(2-aminoethyl)imidazolidin-2-one in 44% yield, m.p. 221-222 C. Found: C,55.69; H,5.63; N,16.55. C23 H28 N6 O5 S requires C,55.18; H,5.64; N,16.79%.
		The following compounds are exemplary of these reactive amine and hydroxy compounds useful in the practice of this invention. 3-Dimethylaminopropylamine, 3-Dimethylaminopropanol, 3-Diethylaminopropylamine, Monoethanolamine, 1-(2-aminoethyl)imidazolidine-2-one, 2-Dimethylaminoethylamine, N-methyl-ethanolamine, 4-Diethylaminobutylamine, 5-Diethylaminopentylamine, ...
	at 190℃; under 11251.1 Torr; for 2h;	General procedure: The process according to the invention can be used to convert various amine molecules into their cyclic urea adducts. This is illustrated in the experiments described below. (0088) Four experiments were carried out: one with aminoethylethanolamine (AEEA), one with diethylenetriamine (DETA), one with triethylenetetramine (TETA) and one with ethylenediamine (EDA) as starting material. For each of these experiments the procedure was the same. (0089) The amine molecule was combined with CO2 in a two-step process. In the first step, the CO2 was loaded into the amine mixture at 100C for 30 min. In the second step of the process, the loaded mixture was heated to a temperature of 190C for two hours in a closed reactor vessel to obtain a mixture of amines and their cyclic urea adducts. The pressure at the end of the second step (at reaction temperature) was below 15 bara for all experiments. After two hours of reaction time, the reaction mixture was cooled down and analyzed using GC- FID, which stands for gas chromatography using a flame ionization detector. (0090) The experimental results are given in Table 2. (0091) (0092) The U-loading was defined as the amount of moles of urea groups in the resulting amine mixture per kilogram of reaction mixture. For all amine molecules a substantial U-loading was attained after step 2 indicating that this procedure is indeed applicable to different amine types (i.e. both ethylene amines as well as ethanol amines). The molar ratio of absorbed CO2 per mole -NH-CH2-CH2-NH- moiety ranges between 0.33 in example 2A and 0.83 in example 2B.

18
[ 6281-42-1 ]
[ 103-71-9 ]
[ 54924-46-8 ]

Yield	Reaction Conditions	Operation in experiment
	In acetone; benzene;	Y = nh. STR5 To a mixture of 6.5 g of commercially available 1-(2-aminoethyl)-2-imidazolidone and 50 ml benzene was added 5.5 ml of phenyl isocyanate. The strongly exothermic reaction was moderated by cooling to 25. The mixture was stirred at 25 for 4 hr. It was cooled in ice and the mixture was filtered. The solid product was crystallized from 250 ml of acetone to give 6.8 g of white 1-[2-(2-oxo-1-imidazolidinyl)ethyl]-3-phenylurea, mp 162-164. IR(Nujol) -- 3.1 mu (NH); 5.9 (C=O). NMR(DMSO-d6) -- m(1H) 8.45 delta (ArNH); m(5H) 6.7-7.5 (aromatic H); m (2H) 5.9-6.3 (NH); m(8H) 3.0-3.5 (CH2).
	In acetone; benzene;	Y=nh STR6 To a mixture of 6.5 g of commercially available 1-(2-aminoethyl)-2-imidazolidone and 50 ml benzene was added 5.5 ml of phenyl isocyanate. The strongly exothermic reaction was moderated by cooling to 25. The mixture was stirred at 25 for 4 hr. It was cooled in ice and the mixture was filtered. The solid product was crystallized from 250 ml of acetone to give 6.8 g of white 1-[2-(2-oxo-1-imidazolidinyl)-ethyl]-3-phenylurea, mp 162- 164. IR(Nujol)-- 3.1mu (NH); 5.9 (C=0) NMR(DMSO-d6)-- m(1H) 8.45 delta (ArNH); m(5H) 6.7-7.5 (aromatic H); m(2H) 5.9-6.3 (NH);m(8H) 3.0-3.5 (CH2).

Reference： [1]Mendeleev Communications,2020,vol. 30,p. 153 - 155
[2]Patent: US3973946,1976,A
[3]Patent: US4032638,1977,A

19
[ 6281-42-1 ]
[ 104-12-1 ]
[ 63874-81-7 ]

Yield	Reaction Conditions	Operation in experiment
	In tetrahydrofuran;	n'=0 STR18 To a mixture of 6.5 g of 1-(2-aminoethyl)-2-imidazolidone in 65 ml of tetrahydrofuran was added 8.0 g of p-chlorophenyl isocyanate with ice cooling to maintain an internal temperature of 25 (exothermic reaction). The mixture was stirred at 25 for 18 hr during which a white solid formed. The mixture was filtered and the solids were washed with petroleum ether. The solid product was crystallized from 100 ml acetone to give 7.5 g of white crystals, m.p. 132-135 C. IR(Nujol)-- 2.9mu (NH); 5.9 (C= O). NMR(DMSO-- d6)-- m(1H) 8.65 delta (NH); AB pattern (4H) 7.33 (aromatic H); m(2H) 6.0-6.4 (NH); m(8H) 3.2 (CH2 N). Calcd for C12 H15 N4 O2 Cl: C, 50.98; H, 5.35; N, 19.82. Found: C, 51.63; H, 5.35; N, 19.30. C, 51.65; H, 5.42; N, 19.47.

Reference： [1]Mendeleev Communications,2020,vol. 30,p. 153 - 155
[2]Patent: US4032638,1977,A

20
[ 111-40-0 ]
[ 6281-42-1 ]

Yield	Reaction Conditions	Operation in experiment
	With urea;	Example C Aminoethylethyleneurea A mixture of 206.4 g of diethylenetriamine (2 moles) and 117.0 g of urea (1.95 moles) was slowly heated to 210C. The evolution of ammonia began when the temperature of the reaction mixture reached 130C. The reaction mixture was then held at 210C for 3 hours before it was distilled under vacuum to afford 132 g of aminoethylethyleneurea. B.P.: 175C (1.5 mm); 1H NMR (DMSO-d6): d 6.3 (s, 1 H), 3.4-2.5 (m, 8 H), 1.4 (s, 1 H).
		Example 1 Synthesis of 2-aminoethyl imidazolidinone In a suitable reactor equipped with an agitator and a reflux condenser, 465 parts by weight of urea and 798 parts by weight of diethylenetriamine were charged. The reaction mix was slowly heated to 140C. Ammonia started to evolve at about 130C. The temperature was slowly raised to 150C. As the evolution of ammonia subsided, vacuum was applied and the remaining ammonia was removed. Product yield was approximately 1000 parts by weight. The product had a viscosity of 6000 cps at 25C and an MEQ/g of 6.5. (MEQ=milliequivalent weight). Gel phase analysis of the product showed approximately 95% purity. The product can be used as is or further purified by vacuum distillation. The major impurity is unreacted diethylenetriamine.

Reference： [1]Patent: EP928820,1999,A2
[2]Patent: EP810996,2002,B1

21
[ 757967-03-6 ]
[ 103-82-2 ]
[ 6281-42-1 ]
[ 100-02-7 ]
[ 623-05-2 ]
[ 124-38-9 ]

Yield	Reaction Conditions	Operation in experiment
	With water;penicillin-G-amidase; In Chremephor EL; dimethyl sulfoxide; at 37℃;pH 7.4;Enzymatic reaction; Aqueous phosphate buffer;Kinetics;	Compounds 1 and 2 (2 mul of a 10 mM stock solution in DMSO) were dissolved in 98 mul of PBS (pH 7.4) to give a final concentration of 200 muM. Compound 3 (2 muL of a 10 mM stock solution in DMSO: Chremephor EL (1:1)) was dissolved in 98 mul of PBS (pH 7.4) to give a final concentration of 200 muM. All solutions were kept at 37 C. A PGA stock solution in PBS (pH 7.4) was used to activate the dendritic compounds. The UV-Visible spectra of p-nitrophenol and of the tested solutions of Compound 1 and 2 in PBS (pH 7.4) were measured in order to determine the optimal wavelength which will be indicative for following the appearance of released p-nitrophenol and the results are depicted in FIG. 5. As shown in FIG. 5, a wavelength of 405 nm, in which p-nitrophenol has a maximal absorption and the dendritic compounds have minimal absorption was found as indicative for the appearance of a released p-nitrophenol. Thus, Compounds 1-3 were incubated with or without PGA in PBS pH 7.4 at 37 C. and the biodegradation of the tested compounds was conveniently monitored by following the formation of 4-nitrophenol with visible spectroscopy at a wavelength of 405 nm. The kinetics of the release of 4-nitrophenol from Compounds 1-3 is shown in FIG. 6. Upon addition of PGA to Compounds 1-3, free 4-nitrophenol was gradually formed, indicating a PGA-induced cleavage of the phenylacetamide substrate and a following degradation that occurs as was predicted. In the absence of PDA, no p-nitrophenol was detected. Expectedly, 4-nitrophenol was released from the G1-dendritic compound (Compound 2) faster then from the G0-dendritic compounds (Compound 1), while the G2-dendritic compound (Compound 3) released it relatively slower. The kinetic constants K(obs) for the three reactions were calculated by linear correlation with the measured plots (e.g., Kobs was calculated as the slop of the linear area of the graphs), and are presented in Table 1 below. Without being bound to any particular theory, it is suggested that the phenomenon of Compound 2 releasing its reporter group faster than Compound 1 occurs since the enzymatic substrate concentration in Compound 2 is twice higher than Compound 1. The following self-cyclization step is relatively fast and therefore, the rate-limiting step is the cleavage of the enzymatic substrate. In Compound 3, additional self-immolative reactions occur in order to complete the release of the reporter group (another intra-cyclization and 1,6-quinone-methide elimination). The overall rate of these reactions is slower than the rate of the enzymatic substrate cleavage and therefore the K(obs) for Compound 3 is relatively smaller.

Reference： [1]Patent: US2006/269480,2006,A1 .Location in patent: Page/Page column 24; sheet 2; 3

22
[ 6281-42-1 ]
[ 1087075-39-5 ]
[ 1034659-31-8 ]

Yield	Reaction Conditions	Operation in experiment
	In 1,4-dioxane; at 85℃; for 4h;	Example 25; l-(2-{4-[7-(3-Amino-pyridin-4-yl)benzo[/?]thiophen-2-yl]-5-fluoropyrimidin-2- ylamino}ethyl)imidazolidin-2-one; Combine N- {4-[2-(2-chloro-5-fluoro-pyrimidin-4-yl)-benzo[]thiophen-7-yl]- pyridin-3-yl}-2,2-dimethyl-propionamide (330 mg, 0.75 mmol), 2-(amino-ethyl)-l,3- dihydro-imidazolone (386 mg, 3.0 mmol), and 1,4-dioxane (6 mL) in a capped vial and heat at 85 0C for 4 hours. Concentrate in vacuo. Dilute the mixture with dichloromethane and water. Wash the organic solution with water. Dry the organic solution over sodium sulfate. Filter and concentrate the solution in vacuo to a dark residue. Purify by column chromatography (dichloromethane to 7 % methanol in dichloromethane) to afford N-[4-(2- {5-fluoro-2-[2-(2-oxo-imidazolidin- 1 -yl)- ethylamino]-pyrimidin-4-yl}-benzo[]thiophen-7-yl)-pyridin-3-yl]-2,2-dimethyl- propionamide.Transfer the amide intermediate to a 40 mL septum capped vial. Add a magnetic stir bar and charge water (20 mL) and concentrated H2SO4 (5 mL) to the vial. Warm the vial to 90 0C in an oil bath for 5 hours. Cool the reaction to room temperature and pass <n="29"/>-28-through an SCX (10 g) column. Elute with water/methanol 1 : 1, then 100 % methanol, then 1 : 1 dichloromethane/methanol, and finally elute the product off with 10 % 2 M ammonia in methanol/90 % dichloromethane. Concentrate in vacuo. Chromatograph on silica (80 g) eluting with gradient of 0 % to 10 % 2 M ammonia/methanol solution in dichloromethane. Dry in vacuum oven at 42 0C for 2 hours to give the title compound (192.6 mg, 48 %) as a gold solid. MS (ES) m/z 450 [M+lf.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 27-28

23
[ 6281-42-1 ]
[ 1034658-89-3 ]
[ 1034657-98-1 ]

Yield	Reaction Conditions	Operation in experiment
93%	In butan-1-ol; at 120℃; for 5h;	Example 1; l-(2-{4-[7-(2-Chloro-pyridin-4-yl)-benzo[£]thiophen-2-yl]pyrimidin-2- ylamino}ethyl)imidazolidin-2-one; Combine 2-chloro-4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]- pyrimidine (9 g, 25.1 mmol) and 2-(amino-ethyl)-l,3-dihydro-imidazol-one (6.4 g, 50.2 mmol) in w-butanol (200 mL) in a pressure vessel. Heat the mixture in an oil bath at 120 0C for 5 hours. Dilute the mixture with chloroform/isopropanol (3/1). Wash the solution with saturated aqueous sodium chloride. Dry it over sodium sulfate. Concentrate the <n="21"/>-20-solution in vacuo to a dark residue. Purify by column chromatography (dichloromethane to 10 % methanol in dichloromethane) to afford the title compound (9 g, 93 %) as a yellow solid. MS (ES) m/z 451 [M+l]+.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 19-20

24
[ 6281-42-1 ]
[ 1034658-91-7 ]
[ 1034658-10-0 ]

Yield	Reaction Conditions	Operation in experiment
	In 1-methyl-pyrrolidin-2-one; at 120℃; for 5h;Microwave irradiation;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20-21

25
[ 6281-42-1 ]
[ 1034658-94-0 ]
[ 1034658-06-4 ]

Yield	Reaction Conditions	Operation in experiment
	In 1-methyl-pyrrolidin-2-one; at 120℃; for 5h;Microwave irradiation;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20-21

26
[ 6281-42-1 ]
[ 1034658-96-2 ]
[ 1034658-00-8 ]

Yield	Reaction Conditions	Operation in experiment
	In 1,4-dioxane; 1-methyl-pyrrolidin-2-one; at 120℃; for 5h;Microwave irradiation;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20

27
[ 6281-42-1 ]
[ 1034658-98-4 ]
[ 1034658-02-0 ]

Yield	Reaction Conditions	Operation in experiment
	In 1,4-dioxane; 1-methyl-pyrrolidin-2-one; at 120℃; for 5h;Microwave irradiation;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20

28
[ 6281-42-1 ]
[ 1034468-16-0 ]
[ 1034658-04-2 ]

Yield	Reaction Conditions	Operation in experiment
	With triethylamine; In butan-1-ol; at 120℃; for 5h;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20

29
[ 6281-42-1 ]
[ 1034659-05-6 ]
[ 1034659-33-0 ]

Yield	Reaction Conditions	Operation in experiment
	In 1,4-dioxane; at 70℃; for 15h;	Example 29; l-(2-{4-[7-(5-Amino-2-fluoropyridin-4-yl)benzo[]thiophen-2-yl]pyrimidin-2- ylamino}ethyl)imidazolidin-2-one; Combine {4-[2-(2-chloro-pyrimidin-4-yl)-benzo[]thiophen-7-yl]-6-fluoro- pyridin-3-yl}-carbamic acid tert-butyl ester (813 mg, 1.77 mmol), 2-(amino-ethyl)-l,3- dihydro-imidazol-one (919 mg, 7.11 mmol), and 1,4-dioxane (22 mL) in a capped vial and heat at 70 0C for 15 hours. Concentrate in vacuo. Dilute the mixture with dichloromethane and water. Wash the organic solution with water. Dry the organic solution over sodium sulfate. Filter and concentrate the solution in vacuo to a dark residue. Purify by column chromatography (dichloromethane to ethyl acetate) to afford [6-fluoro-4-(2-{2-[2-(2-oxo-imidazolidin-l-yl)-ethylamino]-pyrimidin-4-yl}- benzo[£]thiophen-7-yl)-pyridin-3-yl]-carbamic acid tert-butyl ester. Dissolve the [6-fluoro-4-(2-{2-[2-(2-oxo-imidazolidin-l-yl)-ethylamino]- pyrimidin-4-yl}-benzo[£]thiophen-7-yl)-pyridin-3-yl]-carbamic acid tert-butyl ester into dichloromethane and adsorb onto silica gel (10 g) via concentration in vacuo. Dry under high vacuum for 24 hours. Place silica gel into a round bottom flask and heat in a temperature controlled oil bath to 98-99 0C while under high vacuum for 2 hours. Cool to <n="31"/>-30-room temperature. Extract product from silica gel with 10 % 7 N ammonia in methanol/ 90 % dichloromethane. Concentrate in vacuo. Chromatograph on silica eluting with a gradient of 100 % dichloromethane to 7 % 2 N ammonia in methanol/93 % dichloromethane to afford the title compound (65.2 mg, 8.2 %). MS (ES) m/z 450 [M+l]+.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 29-30

30
[ 6281-42-1 ]
[ 1034468-28-4 ]
[ 1034468-55-7 ]

Yield	Reaction Conditions	Operation in experiment
52%	In 1,4-dioxane; at 90℃; for 3h;	Preparation 42; l-{2-[4-(7-Bromo-benzo[]thiophen-2-yl)-5-fluoro-pyrimidin-2-ylamino]-ethyl}- imidazolidin-2-one; Combine l-(2-aminoethyl)-2-imidazolone (100 g, 774 mmol) with 4-(7-bromo- benzo[]thiophen-2-yl)-2-chloro-5-fluoro-pyrimidine (90 g, 262 mmol) in 1,4-dioxane (650 mL) and heat to 90 0C with stirring under nitrogen for 3 hours. Cool the reaction to room temperature. Filter and wash the solid with water (3 x 500 mL) and diethyl ether (500 mL). Vacuum-dry at 50 0C to give the title compound (59.2 g, 52 %) as a yellow solid. MS (ES) m/z 436 [M+lf.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 17

31
[ 6281-42-1 ]
[ 1034659-08-9 ]
[ 1034658-08-6 ]

Yield	Reaction Conditions	Operation in experiment
	With triethylamine; In butan-1-ol; at 120℃; for 5h;	Prepare the following examples essentially according to the preparation of l-(2- {4-[7-(2-chloro-pyridin-4-yl)-benzo[]thiophen-2-yl]pyrimidin-2-ylamino}-ethyl)- imidazolidin-2-one using the appropriate starting material.

Reference： [1]Patent: WO2008/76704,2008,A1 .Location in patent: Page/Page column 20-21

32
[ 6281-42-1 ]
[ 1034468-08-0 ]
[ 1034466-20-0 ]

Yield	Reaction Conditions	Operation in experiment
63%	With triethylamine; In butan-1-ol; at 120℃; for 15h;	Example 1; l-(2-{4-[7-(5-((Dimethylamino)methyl)-2-fluoro-pyridin-4-yl)benzo[]thiophen-2-yl]-5- fluoropyrimidin-2-ylamino}ethyl)imidazolidin-2-one; Combine {4-[2-(2-chloro-5-fluoro-pyrimidin-4-yl)-benzo[/?]thiophen-7-yl]-6-fluoro- pyridin-3-ylmethyl}-dimethyl-amine (0.25 g, 0.59 mmol) and triethylamine (0.25 mL, 1.78 mmol) in w-butanol (8.0 mL). Add l-(2-aminoethyl) imidazolidin-2-one (0.23 g, 1.78 mmol). Heat the reaction mixture at 120 C overnight (15 hours), then cool to room temperature. Dilute the reaction mixture with ethyl acetate, and wash with water and saturated aqueous sodium chloride. Separate the organic layer from aqueous layer and dry over MgSO4. After filtration, remove the organic solvent to give a crude. Purify the crude by column chromatography (0.5 % to 10 % 2 N NH3 in methanol solution/dichloromethane) to afford the title compound (0.19 g, 63 %). MS (ES) m/z 510 [M+lf.

Reference： [1]Patent: WO2008/76705,2008,A1 .Location in patent: Page/Page column 31

33
[ 6281-42-1 ]
[ 1034468-45-5 ]
[ 1034468-65-9 ]

Yield	Reaction Conditions	Operation in experiment
49%	In butan-1-ol; at 120℃; for 4 - 5h;	Preparation 91; l-(2-[4-[7-(3-Trimethylsilanylethynyl-pyridin-4-yl)-benzo[/?]-thiophen-2-yl]-pyrimidin-2- yl-amino)-ethyl imidazolidin-2-one; Add 2-chloro-4-[7-(3-trimethylsilanylethynyl-pyridin-4-yl)-benzo[]-thiophen-2- yl]- pyrimidine (0.180 g, 0.4 mmol) to a sealed tube and add r°-butanol (2 mL) to it. Add <n="29"/>N-2-amino ethyl imidazolidin-2-one (0.103 g, 0.8 mmol). Seal the tube and heat in an oil bath for 4-5 hours at 120 0C. Concentrate the reaction mixture under reduced pressure and purify the crude through column chromatography. Yield (0.1 g, 49 %); 1H nuMR (400 MHz, DMSO -d6) delta 8.832 (s, IH), 8.725 (d, J= 5.2 Hz, IH), 8.394 (s, IH), 8.369 (s, IH), 8.015 (d, J= 8.8 Hz IH), 7.711 (d, J= 5.2 Hz, IH), 7.552 (m, 2H), 7.356 (s, IH), 7.272 (d, J= 4.8 Hz, IH), 6.288 (s, IH), 3.185 (m, 4H), 0.286 (s, 9H); MS (ES) m/z 513

Reference： [1]Patent: WO2008/76705,2008,A1 .Location in patent: Page/Page column 27-28

34
[ 6281-42-1 ]
[ 90826-32-7 ]
[ 137559-77-4 ]

Yield	Reaction Conditions	Operation in experiment
83%	1,3-diacetoxy-1,1,3,3-tetrabutyldistannoxane; at 140℃; under 30 Torr; for 3h;	A mixture of 3.0 g (0.013 moles) m-TMU, 1.93 g (0.015 mole) AEEU and 80 mg TK-1 tin catalyst was heated in a 140[deg.] C. bath under 30 mm Hg pressure for 3 hrs. The reaction mixture was allowed to cool and then dissolved in 20 ml of chloroform. The chloroform solution was extracted with 20 ml of water and dried over potassium carbonate. Removal of solvent left a white solid residue which weighed 3.5 g, 83% yield. M.P.: 120[deg.]-125[deg.] C.; <1>H-NMR (CDCl3): [delta]7.2-7.6 (m, 4 H); 5.55 (s, 1 H); 5.4 (s, 1 H); 5.0-5.2 (m, 2 H); 4.8 (s, 1 H); 3.0-3.4 (m, 8 H); 2.15 (s, 3 H); 1.6 (s, 6 H)

Reference： [1]Patent: US6630599,2003,B1 .Location in patent: Page/Page column 11; 12

35
[ 6281-42-1 ]
[ 295338-15-7 ]
C₂₈H₄₃N₉O₆ [ No CAS ]

Reference： [1]Bioorganic and Medicinal Chemistry Letters,2008,vol. 18,p. 2536 - 2539

36
[ 6281-42-1 ]
C₂₄H₂₁Cl₂N₅O₂S₂ [ No CAS ]
[ 1033352-68-9 ]

Reference： [1]Bioorganic and Medicinal Chemistry Letters,2008,vol. 18,p. 2825 - 2829

37
[ 6281-42-1 ]
C₂₅H₂₂ClN₅OS [ No CAS ]
[ 1033352-74-7 ]

Reference： [1]Bioorganic and Medicinal Chemistry Letters,2008,vol. 18,p. 2825 - 2829

38
[ 6281-42-1 ]
C₂₃H₁₇ClF₃N₅OS [ No CAS ]
[ 1033352-80-5 ]

Reference： [1]Bioorganic and Medicinal Chemistry Letters,2008,vol. 18,p. 2825 - 2829

39
[ 6281-42-1 ]
C₂₅H₂₀ClF₃N₆OS [ No CAS ]
[ 1033352-62-3 ]

Reference： [1]Bioorganic and Medicinal Chemistry Letters,2008,vol. 18,p. 2825 - 2829

40
[ 6281-42-1 ]
[ 1181814-94-7 ]
[ 1181815-09-7 ]

Reference： [1]Journal of Medicinal Chemistry,2009,vol. 52,p. 5005 - 5008

41
[ 6281-42-1 ]
[ 1240186-30-4 ]
C₂₁H₂₈ClN₅O₃ [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	With N-ethyl-N,N-diisopropylamine; In butan-1-ol; at 120℃; for 72h;	A mixture of Intermediate 23 (1.0 g, 2.9 mmol), l-(2-aminoethyl)imidazolidin-2- one (0.5 g, 3.9 mmol) and DIPEA (0.8 mL, 5.8 mmol) in w-butanol (10 mL) was heated at 1200C for 72 h. After cooling, the reaction mixture was partitioned between Et2O (200 mL) and water (100 mL). The organic layer was washed with water (3 x 100 mL) and brine (100 mL), separated, dried (MgSO4), filtered and concentrated in vacuo. The residue was purified by column chromatography (SiO2, 5% MeOH in DCM) to give a pale yellow solid. This was dissolved in DCM (20 mL), treated with TFA (5 mL) and stirred for 4 h at r.t. After quenching with 2M NaOH solution (30 mL), the organic layer was washed with water (3 x 10 mL), separated, dried (MgSO4), filtered and concentrated in vacuo to give an orange oil (0.8 g, 82%). A portion of this oil (100 mg, 0.3 mmol), 4- chloropyrido[3,2-(i]pyrimidine (55 mg, 0.33 mmol) and DIPEA (100 mg, 0.78 mmol) in rt-butanol (2 mL) was heated at 12O0C for 18 h. The solvent was removed in vacuo and the residue was purified by preparative HPLC to give the title compound (70 mg, 48%) as a pale yellow solid. deltaH (CDCl3) 8.70-8.66 (2H, m), 8.15-8.09 (IH, m), 7.90 (IH, s), 7.67 (IH, dd, J 8.48, 4.25 Hz), 7.62 (IH, dd, J7.54, 1.39 Hz), 7.53-7.46 (IH, m), 7.33 (IH, d, J9.01 Hz), 7.10 (IH, t, Jl.15 Hz), 6.74 (IH, s), 5.75-5.64 (IH, m), 4.55 (IH, s), 3.98- 3.87 (IH, m), 3.76-3.65 (IH, m), 3.63-3.42 (4H, m), 3.29-3.13 (2H, m), 1.82 (3H, d, J 6.78 Hz). LCMS (ES+) 463 (M+H)+, 2.98 minutes {Method I).

Reference： [1]Patent: WO2010/92340,2010,A1 .Location in patent: Page/Page column 102-103

42
[ 6281-42-1 ]
[ 1240186-20-2 ]
[ 1240187-37-4 ]

Yield	Reaction Conditions	Operation in experiment
17%	With N-ethyl-N,N-diisopropylamine; In butan-1-ol; at 120℃; for 72h;	Intermediate 15 (324 mg, 1.0 mmol), l-(2-aminoethyl)imidazolidin-2-one (260 mg, 2.0 mmol), DIPEA (270 mg, 2.0 mmol) and n-butanol (5.0 mL) were combined in a sealed tube and heated to 12O0C for 72 h. After cooling, the mixture was dissolved in a 1 :1 mixture OfEt2O and EtOAc (200 mL) and washed with saturated brine (3 x 50 mL). The organic layer was dried (MgSO4), filtered and concentrated in vacuo. Purification by column chromatography (SiO2, 0-5% MeOH in DCM) gave a yellow solid (76 mg, 17%). This was dissolved in DCM (5 mL) and treated with TFA (1 mL) and the mixture stirred for 4 h at r.t. before being quenched with 2M NaOH solution (30 mL). The organic layer was washed with water (2 x 10 mL), dried (MgSO4), filtered and concentrated in vacuo to give a pale orange gum (55 mg, 94%). This was combined with 7-chloropyrazolo[l,5-alpha]- pyrimidine (38 mg, 0.22 mmol) and DIPEA (100 mg, 0.78 mmol) in n-butanol (2 mL) and the mixture heated at 1200C for 16 h. After cooling, the mixture was dissolved in a 1 :1 mixture OfEt2O and EtOAc (100 mL) and washed with saturated brine (3 x 10 mL). The organic layer was separated, dried (MgSO4), filtered and concentrated in vacuo. Purification of the residue by preparative HPLC gave the title compound (6 mg, 7.8%) as a white solid. deltaH (MeOD-d0 8.16 (IH, d, J2.32 Hz), 8.10 (IH, d, J5.40 Hz), 7.95 (IH, s), 7.60 (IH, dd, J8.85, 6.33 Hz), 7.31 (IH, dd, J 11.11, 2.53 Hz), 6.97 (IH, td, J8.72, 2.56 Hz), 6.49 (IH, d, J2.33 Hz), 5.93 (IH, d, J5.43 Hz), 5.06 (IH, q, J6.73 Hz), 4.00- 3.90 (IH, m), 3.83-3.73 (IH, m), 3.72-3.52 (4H, m), 3.32-3.26 (2H, m), 1.78 (3H, d, J 6.74 Hz). LCMS (ES+) 435 (M+H)+, 8.93 minutes {Method 9).

Reference： [1]Patent: WO2010/92340,2010,A1 .Location in patent: Page/Page column 106

43
[ 6281-42-1 ]
[ 76-05-1 ]
[ 43045-16-5 ]
1-(2-(4-(4-fluorophenyl)thiazol-2-ylamino)ethyl)imidazolidin-2-one trifluoroacetate [ No CAS ]