[ CAS No. 4275-43-8 ]

Name: 4275-43-8|1,3-Diphenylpropan-2-amine|97%
Brand: Ambeed
SKU: A123754
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Cat. No.: {[proInfo.prAm]}

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Quality Control of [ 4275-43-8 ]

COA NMR CNMR HPLC LC-MS

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SDS Specification

Alternatived Products of [ 4275-43-8 ]

Product Details of [ 4275-43-8 ]

CAS No. :	4275-43-8	MDL No. :	MFCD00449548
Formula :	C₁₅H₁₇N	Boiling Point :	-
Linear Structure Formula :	-	InChI Key :	BWYYVSNVUCFQQN-UHFFFAOYSA-N
M.W :	211.30	Pubchem ID :	77960
Synonyms :

Calculated chemistry of [ 4275-43-8 ]

Physicochemical Properties

Num. heavy atoms :	16
Num. arom. heavy atoms :	12
Fraction Csp3 :	0.2
Num. rotatable bonds :	4
Num. H-bond acceptors :	1.0
Num. H-bond donors :	1.0
Molar Refractivity :	68.22
TPSA :	26.02 Å²

Pharmacokinetics

GI absorption :	High
BBB permeant :	Yes
P-gp substrate :	No
CYP1A2 inhibitor :	Yes
CYP2C19 inhibitor :	Yes
CYP2C9 inhibitor :	No
CYP2D6 inhibitor :	Yes
CYP3A4 inhibitor :	No
Log Kp (skin permeation) :	-5.21 cm/s

Lipophilicity

Log Po/w (iLOGP) :	2.66
Log Po/w (XLOGP3) :	3.35
Log Po/w (WLOGP) :	2.8
Log Po/w (MLOGP) :	3.6
Log Po/w (SILICOS-IT) :	3.57
Consensus Log Po/w :	3.2

Druglikeness

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

Water Solubility

Log S (ESOL) :	-3.55
Solubility :	0.0593 mg/ml ; 0.000281 mol/l
Class :	Soluble
Log S (Ali) :	-3.57
Solubility :	0.0564 mg/ml ; 0.000267 mol/l
Class :	Soluble
Log S (SILICOS-IT) :	-5.42
Solubility :	0.000803 mg/ml ; 0.0000038 mol/l
Class :	Moderately soluble

Medicinal Chemistry

PAINS :	0.0 alert
Brenk :	0.0 alert
Leadlikeness :	1.0
Synthetic accessibility :	1.26

Safety of [ 4275-43-8 ]

Signal Word:	Danger	Class:	8
Precautionary Statements:	P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P310-P330-P332+P313-P362-P403+P233-P405-P501	UN#:	3259
Hazard Statements:	H302-H312-H315-H318-H332-H335	Packing Group:	Ⅲ
GHS Pictogram:

Application In Synthesis of [ 4275-43-8 ]

* 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.

Downstream synthetic route of [ 4275-43-8 ]

[ 4275-43-8 ] Synthesis Path-Downstream 1~50

1
[ 75-44-5 ]
[ 4275-43-8 ]
[ 810-45-7 ]

Yield	Reaction Conditions	Operation in experiment
	With diethyl ether

Reference： [1]Jones; Scott [Journal of the American Chemical Society, 1922, vol. 44, p. 415]

2
[ 1788-31-4 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
94%	With sodium tetrahydroborate; titanium tetrachloride In 1,2-dimethoxyethane for 14h; Ambient temperature;
86%	With sodium In ethanol Heating;
	With sodium amalgam; acetic acid

	With ethanol; nickel Hydrogenation;
	With ethanol elektrolytische Reduktion an Bleikathoden;
	With ethanol; sodium
	With methanol; nickel Hydrogenation;
	With diborane In tetrahydrofuran; diethylene glycol dimethyl ether at 105 - 110℃;
	With lithium aluminium tetrahydride In tetrahydrofuran

Reference： [1]Kano, Shinzo; Tanaka, Yasuyuki; Sugino, Eiichi; Hibino, Sstoshi [Synthesis, 1980, # 9, p. 695 - 697]
[2]Riddell, Frank G.; Rogerson, Martin [Journal of the Chemical Society. Perkin Transactions 2 (2001), 1997, # 2, p. 249 - 255]
[3]Jacobsen et al. [Skandinavisches Archiv fur Physiologie, 1938, vol. 79, p. 258,279]
[4]Exner et al. [Chemicke Listy, 1954, vol. 48, p. 65,68][Chem.Abstr., 1955, p. 1664] Kametano; Nomura [Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1954, vol. 74, p. 413,414,416][Chem.Abstr., 1955, p. 5342]
[5]Kaplansky [Chemische Berichte, 1927, vol. 60, p. 1843]
[6]Noyes [American Chemical Journal, 1892, vol. 14, p. 229]
[7]Sasa [Yuki Gosei Kagaku Kyokaishi, 1954, vol. 12, p. 133][Chem.Abstr., 1957, p. 2780]
[8]Feuer,H.; Braunstein,D.M. [Journal of Organic Chemistry, 1969, vol. 34, # 6, p. 1817 - 1821]
[9]Kotera,K. et al. [Tetrahedron, 1968, vol. 24, p. 6177 - 6184]

3
[ 4275-43-8 ]
[ 77414-34-7 ]

Reference： [1]Koelsch [Journal of the American Chemical Society, 1945, vol. 67, p. 17,18]

4
[ 4275-43-8 ]
[ 101083-66-3 ]

Yield	Reaction Conditions	Operation in experiment
	With 1,4-dioxane; ruthenium at 130 - 140℃; Hydrogenation;

Reference： [1]Edgerton et al. [Journal of the American Pharmaceutical Association (1912), 1959, vol. 48, p. 320,323]

5
[ 788-09-0 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
	With hydrogenchloride
	With sulfuric acid
	With hydrogenchloride for 16h; Heating; Yield given;

Reference： [1]Dey; Ramanathan [Proceedings of the National Institute of Sciences of India, 1943, vol. 9, p. 193,222]
[2]Koelsch [Journal of the American Chemical Society, 1945, vol. 67, p. 1718]
[3]Grunewald, Gary L.; Monn, James A.; Rafferty, Michael F,; Borchardt, Ronald T.; Krass, Polina [Journal of Medicinal Chemistry, 1982, vol. 25, # 10, p. 1248 - 1250]

6
[ 4275-43-8 ]
[ 98-09-9 ]
[ 78515-33-0 ]

Yield	Reaction Conditions	Operation in experiment
	With sodium hydroxide

Reference： [1]Gensler; Rockett [Journal of the American Chemical Society, 1955, vol. 77, p. 3262]

7
[ 4275-43-8 ]
[ 103-80-0 ]
[ 77414-37-0 ]

Yield	Reaction Conditions	Operation in experiment
	With sodium hydroxide
	With sodium hydroxide at 0℃; for 2h;

Reference： [1]Dey; Ramanathan [Proceedings of the National Institute of Sciences of India, 1943, vol. 9, p. 193,222]
[2]Nagubandi, Sreeramulu [Organic Mass Spectrometry, 1980, vol. 15, # 10, p. 535 - 538]

8
[ 102-04-5 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
81%	With nickel(II) tetrafluoroborate hexahydrate; ammonia; hydrogen; bis(2-diphenylphosphinoethyl)phenylphosphine In 2,2,2-trifluoroethanol at 120℃; for 24h; chemoselective reaction;
67.7%	With ammonium acetate; sodium cyanoborohydride In methanol at 0 - 25℃; for 3h;	8.1 Step 1: 1,3-Diphenylpropan-2-amine (2): To a solution of dibenzyl ketone (500 mg, 2.38 mmol) in MeOH (10 mL) was added ammonium acetate (1.83 g, 23.78 mmol) and NaBH3CN (300 mg, 4.76 mmol) at 0 °C and the mixture was stirred at 25 °C for 3 hours. The reaction mixture was quenched with iN aqueous NaOH solution and extracted with EtOAc twice. The combined organic layers were washed with brine, dried over Na2SO4, filtered and concentrated todryness. The residue was purified by column chromatography via silica gel (eluted with DCM:MeOH= 200: 1 to 20: 1) to afford compound 2 (340 mg, yield 67.7%) as colorless oil. LC/MS (ESI) m/z: 212(M+H)t
	With ammonium formate at 220℃; anschliessend Behandeln mit aethanol.Kalilauge;

	With methanol; ammonia; nickel Hydrogenation;
	Multi-step reaction with 2 steps 1: 175 °C 2: aq.-ethanolic sulfuric acid
	With ammonium acetate; sodium cyanoborohydride In methanol at 20℃; for 40h;
	Stage #1: 1,3-Diphenylpropanone With ammonium acetate In methanol at 20℃; for 1.5h; Inert atmosphere; Stage #2: With methanol; sodium cyanoborohydride at 20℃; for 56h; Inert atmosphere;

Reference： [1]Beller, Matthias; Chandrashekhar, Vishwas G.; Jagadeesh, Rajenahally V.; Jiao, Haijun; Murugesan, Kathiravan; Wei, Zhihong [Chemical Science, 2020, vol. 11, # 17, p. 4332 - 4339]
[2]Current Patent Assignee: ASTRAZENECA PLC - WO2018/160889, 2018, A1 Location in patent: Page/Page column 715; 716
[3]Ogata; Niinobu [Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1942, vol. 62, p. 152,153,158;dtsch.Ref.S.47][Chem.Abstr., 1951, p. 1728]
[4]Sasa [Yuki Gosei Kagaku Kyokaishi, 1954, vol. 12, p. 105,107][Chem.Abstr., 1957, p. 2780]
[5]Koelsch [Journal of the American Chemical Society, 1945, vol. 67, p. 1718]
[6]Eey, Stanley T.-C.; Lear, Martin J. [Chemistry - A European Journal, 2014, vol. 20, # 36, p. 11556 - 11573]
[7]Han, Hui; Zhang, Tao; Yang, Shang-Dong; Lan, Yu; Xia, Ji-Bao [Organic Letters, 2019, vol. 21, # 6, p. 1749 - 1754]

9
[ 556-89-8 ]
[ 4275-43-8 ]
[ 38545-95-8 ]

Yield	Reaction Conditions	Operation in experiment
43%	In water at 70℃; for 1h;
	In water

Reference： [1]Bakibaev, S. S.; Akhmedzhanov, R. R.; Filimonov, V. D.; Novocheeva, T. P.; Saratikov, A. S.; et al. [Pharmaceutical Chemistry Journal, 1993, vol. 27, # 9, p. 631 - 634][Khimiko-Farmatsevticheskii Zhurnal, 1993, vol. 27, # 9, p. 27 - 29]
[2]Pechenkin,A.G. et al. [Pharmaceutical Chemistry Journal, 1972, vol. 6, # 7, p. 451 - 453][Khimiko-Farmatsevticheskii Zhurnal, 1972, vol. 6, # 7, p. 29 - 31]

10
[ 71847-26-2 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
	With hydrogenchloride In tetrahydrofuran

Reference： [1]Zwierzak,A.; Slusarska,E. [Synthesis, 1979, p. 691 - 693]

11
[ 4275-43-8 ]
[ 2004-06-0 ]
[ 57294-70-9 ]

Yield	Reaction Conditions	Operation in experiment
46%	With triethylamine In ethanol Heating;

Reference： [1]Kusachi, Shozo; Thompson, Robert D.; Bugni, William J.; Yamada, Nobuyuki; Olsson, R. A. [Journal of Medicinal Chemistry, 1985, vol. 28, # 11, p. 1636 - 1643]

12
[ 4275-43-8 ]
[ 98-88-4 ]
[ 77414-34-7 ]

Yield	Reaction Conditions	Operation in experiment
82%	With sodium hydroxide In water at 0℃; for 1h;
	With sodium hydroxide at 0℃; for 2h;

Reference： [1]Nagubandi, Sreeramulu; Fodor, G. [Journal of Heterocyclic Chemistry, 1980, vol. 17, p. 1457 - 1463]
[2]Nagubandi, Sreeramulu [Organic Mass Spectrometry, 1980, vol. 15, # 10, p. 535 - 538]

13
[ 20924-87-2 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
	With hydrogen In water

Reference： [1]Kotera,K. et al. [Tetrahedron, 1968, vol. 24, p. 6177 - 6184]

14
[ 4275-43-8 ]
C₁₈H₂₉NO₆ [ No CAS ]
(2S)-[1-(3,3-dimethyl-2-oxopentanoyl)(2-piperidyl)]-N-(3,3-diphenylprop-1-yl)formamide [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	In dichloromethane at 0℃; for 1h;

Reference： [1]Hamilton, Gregory S.; Wu, Yong-Qian; Limburg, David C.; Wilkinson, Douglas E.; Vaal, Mark J.; Li, Jia-He; Thomas, Christine; Huang, Wei; Sauer, Hansjorg; Ross, Douglas T.; Soni, Raj; Chen, Yi; Guo, Hongshi; Howorth, Pamela; Valentine, Heather; Liang, Shi; Spicer, Dawn; Fuller, Mike; Steiner, Joseph P. [Journal of Medicinal Chemistry, 2002, vol. 45, # 16, p. 3549 - 3557]

15
[ 4275-43-8 ]
[ 959853-36-2 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: toluene; methanol 2: sodium borohydride / methanol

Reference： [1]Hamza, Daniel; Stocks, Michael J.; Décor, Anne; Pairaudeau, Garry; Stonehouse, Jeffrey P. [Synlett, 2007, # 16, p. 2584 - 2586]

16
[ 4275-43-8 ]
C₂₇H₃₀N₂ [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 3 steps 1: toluene; methanol 2: sodium borohydride / methanol 3: 78 percent / dimethylformamide; H₂O / 4 h / 110 °C

Reference： [1]Hamza, Daniel; Stocks, Michael J.; Décor, Anne; Pairaudeau, Garry; Stonehouse, Jeffrey P. [Synlett, 2007, # 16, p. 2584 - 2586]

17
[ 102-04-5 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: 3 h / 165 °C 2: 6N aq. HCl / 16 h / Heating
	Multi-step reaction with 2 steps 1: 175 °C 2: aqueous hydrochloric acid

Reference： [1]Grunewald, Gary L.; Monn, James A.; Rafferty, Michael F,; Borchardt, Ronald T.; Krass, Polina [Journal of Medicinal Chemistry, 1982, vol. 25, # 10, p. 1248 - 1250]
[2]Dey; Ramanathan [Proceedings of the National Institute of Sciences of India, 1943, vol. 9, p. 193,222]

18
[ 4275-43-8 ]
[ 77988-88-6 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: 82 percent / 15percent sodium hydroxide / H₂O / 1 h / 0 °C 2: 80 percent / polyphosphoric ester, phenyl sulfide / CHCl₃ / 60 h / Ambient temperature

Reference： [1]Nagubandi, Sreeramulu; Fodor, G. [Journal of Heterocyclic Chemistry, 1980, vol. 17, p. 1457 - 1463]

19
[ 1589-82-8 ]
[ 4275-43-8 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: benzene; diethyl ether 2: HCl / tetrahydrofuran

Reference： [1]Zwierzak,A.; Slusarska,E. [Synthesis, 1979, p. 691 - 693]

20
[ 5711-28-4 ]
[ 4275-43-8 ]
[ 541-41-3 ]
N-[1-(benzyl)-2-(phenyl)ethyl]-cis-2-octyl-cyclopropanoctanamide [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	With hydrogenchloride; aq. sodium hydroxide; triethylamine In dichloromethane	7 N-[1-(benzyl)-2-(phenyl)-ethyl]-cis-2-Octyl-cyclopropanoctanamide STR19 EXAMPLE 7 N-[1-(benzyl)-2-(phenyl)-ethyl]-cis-2-Octyl-cyclopropanoctanamide STR19 To a cooled solution of 2.0 g (cis)-2-octylcyclopropanoctanoic acid in 70 ml methylene chloride at -20° is added first 0.707 g triethylamine and then dropwise 0.732 g ethylchloroformate. The reaction mixture is then allowed to come to room temperature and stirred for 1 hours. Then 1.5 g of 1-benzyl-2-(phenyl)ethylamine is added, and the reaction mixture stirred for 16 hours. The reaction mixture is then extracted a few times with 2 N hydrochloric acid, then with 2 N aq. sodium hydroxide sol. and washed several times with saturated aq. sodium chloride. The organic phase is then dried over anh. sodium sulphate filtered and evaporated i.v. to dryness to obtain a residue, which upon crystallization from pentane yields the title product (m.p. 40°-45°).

Reference： [1]Current Patent Assignee: NOVARTIS AG; Sandoz (in: Novartis) - US4248893, 1981, A

21
[ 4275-43-8 ]
[ 549505-59-1 ]
[ 1041850-42-3 ]

Yield	Reaction Conditions	Operation in experiment
14.3%	at 160℃; for 22h; Inert atmosphere;

Reference： [1]Laufer, Stefan A.; Hauser, Dominik R. J.; Domeyer, David M.; Kinkel, Katrin; Liedtke, Andy J. [Journal of Medicinal Chemistry, 2008, vol. 51, # 14, p. 4122 - 4149]

22
[ 4275-43-8 ]
benzhydrylidene aza-propargylglycinyl-proline hydrochloride [ No CAS ]
[ 1234782-75-2 ]

Yield	Reaction Conditions	Operation in experiment
16.7 mg	Stage #1: benzhydrylidene aza-propargylglycinyl-proline hydrochloride With 4-methyl-morpholine; isobutyl chloroformate In tetrahydrofuran at -15℃; for 0.0833333h; Inert atmosphere; Stage #2: 1-benzyl-2-phenylethylamine In tetrahydrofuran at -15℃; for 2h; Inert atmosphere;

Reference： [1]Location in patent: experimental part Bourguet, Carine B.; Proulx, Caroline; Klocek, Sophie; Sabatino, David; Lubell, William D. [Journal of Peptide Science, 2010, vol. 16, # 6, p. 284 - 296]

23
[ 4275-43-8 ]
benzhydrylidene aza-allylglycinyl-proline hydrochloride [ No CAS ]
[ 1234782-93-4 ]

Yield	Reaction Conditions	Operation in experiment
39.7 mg	Stage #1: benzhydrylidene aza-allylglycinyl-proline hydrochloride With 4-methyl-morpholine; isobutyl chloroformate In tetrahydrofuran at -15℃; for 0.0833333h; Inert atmosphere; Stage #2: 1-benzyl-2-phenylethylamine In tetrahydrofuran at -15℃; for 2h; Inert atmosphere;

24
[ 4275-43-8 ]
benzhydrylidene aza-phenylalaninyl-proline hydrochloride [ No CAS ]
[ 1234782-82-1 ]

Yield	Reaction Conditions	Operation in experiment
47 mg	Stage #1: benzhydrylidene aza-phenylalaninyl-proline hydrochloride With 4-methyl-morpholine; isobutyl chloroformate In tetrahydrofuran at -15℃; for 0.0833333h; Inert atmosphere; Stage #2: 1-benzyl-2-phenylethylamine In tetrahydrofuran at -15℃; for 2h; Inert atmosphere;

25
[ 4275-43-8 ]
benzhydrylidene aza-alaninyl-proline hydrochloride [ No CAS ]
[ 1234782-83-2 ]

Yield	Reaction Conditions	Operation in experiment
11 mg	Stage #1: benzhydrylidene aza-alaninyl-proline hydrochloride With 4-methyl-morpholine; isobutyl chloroformate In tetrahydrofuran at -15℃; for 0.0833333h; Inert atmosphere; Stage #2: 1-benzyl-2-phenylethylamine In tetrahydrofuran at -15℃; for 2h; Inert atmosphere;

26
[ 766-77-8 ]
[ 622-29-7 ]
[ 4275-43-8 ]
N-benzylidenemethylamine [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	With N-methyl acridinium tetra(3,5-dichlorophenyl)borate In dimethylsulfoxide-d6; 1,2-dichloro-benzene at 100℃; for 24h; Inert atmosphere;

Reference： [1]Clark, Ewan R.; Ingleson, Michael J. [Angewandte Chemie - International Edition, 2014, vol. 53, # 42, p. 11306 - 11309][Angew. Chem., 2014, vol. 126, # 42, p. 11488 - 11491,4]

27
[ 1914-59-6 ]
[ 4275-43-8 ]
(E)-N,N-dibenzyl-2-oxo-4-phenylbut-3-enamide [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
47%	With benzotriazol-1-ol; triethylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide for 12h;	Step 2⁴: General procedure: To a solution of M-1 (0.81 g, 4.6 mmol), HATU (2.1 g, 5.5 mmol) and HOBt (0.7 g, 5.5 mmol) indry DMF was added the amine or amine hydrochloride (0.6 g, 5.1 mmol) and triethylamine (0.5 g,5.5 mmol) under 0 °C. The mixture was stirred overnight, evaporated and diluted with ethyl acetateor dichloromethane. The organic layer was washed with 1N HCl and finally brine, dried overNa2SO4 and purified by flash chromatography using (petroleum ether/EtOAc = 30:1) as eluent,affording α-keto-β-enamide. (55-68% yield).

Reference： [1]Wang, Simin; Yu, Yuena; Wen, Jialin; Zhang, Xumu [Synlett, 2018, vol. 29, # 16, p. 2203 - 2207]

28
[ 4275-43-8 ]
[ 1306734-44-0 ]
tert-butyl (1R,3S,5R)-3-((1,3-diphenylpropan-2-yl)carbamoyl)-5-methyl-2-azabicyclo[3.1.0]hexane-2-carboxylate [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
76.4%	With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 0 - 25℃; for 2h;	8.2 Step 2: tert-Butyl(1R,35,5R)-3-((1 ,3-diphenylpropan-2-yl)carbamoyl)-5-methyl-2-azabicycloj3.1.Ojhexane-2-carboxylate (3): To a mixture of 2 (70 mg, 0.33 mmol) and(1 R, 35, 5R)-2-(tert-butoxycarbonyl)-5 -methyl-2-azabicyclo[3. 1. 0]hexane-3 -carboxylicacid (88 mg, 0.36 mmol) in DMF (3 mL) was added DIPEA (86 mg, 0.66 mmol) and HATU(252 mg, 0.66 mmol) at 0 °C and the mixture was stirred at 25 °C for 2 hours. The mixture wasdiluted with ethyl acetate, washed with water and brine, dried over Na2SO4, filtered andconcentrated to dryness. The residue was purified by column chromatography via silica gel (elutedwith petroleum ether: EtOAc= 50: 1 to 1: 1) to afford compound 3 (110 mg, yield 76.4%) as colorless oil. LC/MS (ESI) m/z: 435(M+H)t

Reference： [1]Current Patent Assignee: ASTRAZENECA PLC - WO2018/160889, 2018, A1 Location in patent: Page/Page column 715; 716

29
[ 4275-43-8 ]
(1R,3S,5R)-N-(1,3-diphenylpropan-2-yl)-5-methyl-2-azabicyclo[3.1.0]hexane-3-carboxamide [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 h / 0 - 25 °C 2: trifluoroacetic acid / dichloromethane / 4 h / 0 - 25 °C

Reference： [1]Current Patent Assignee: ASTRAZENECA PLC - WO2018/160889, 2018, A1

30
[ 4275-43-8 ]
(S)-3-benzyl-2-neopentyl-3,4-dihydroisoquinolin-1(2H)-one [ No CAS ]
3-benzyl-2-neopentyl-3,4-dihydroisoquinolin-1(2H)-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: methanol; sodium cyanoborohydride / 20 °C 2: palladium dichloride; L-Pyroglutamic acid; (S)-[1,1']-binaphthalenyl-2,2'-diol; copper(II) bis(trifluoromethanesulfonate); silver carbonate / acetonitrile / 12 h / 80 °C / 760.05 Torr / Schlenk technique