[ CAS No. 1187932-25-7 ] {[proInfo.proName]}

Name: 1187932-25-7|(R)-tert-Butyl (1-(3-bromophenyl)ethyl)carbamate|97%
Brand: Ambeed
SKU: A350430
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2D 3D

Structure of 1187932-25-7 * Storage: {[proInfo.prStorage]}

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Quality Control of [ 1187932-25-7 ]

COA NMR CNMR HPLC LC-MS

Related Doc. of [ 1187932-25-7 ]

SDS Specification

Alternatived Products of [ 1187932-25-7 ]

Product Details of [ 1187932-25-7 ]

CAS No. :	1187932-25-7	MDL No. :	MFCD12913696
Formula :	C₁₃H₁₈BrNO₂	Boiling Point :	-
Linear Structure Formula :	-	InChI Key :	WWNQMGYJYMXOEU-SECBINFHSA-N
M.W :	300.19	Pubchem ID :	67959607
Synonyms :

Calculated chemistry of [ 1187932-25-7 ]

Physicochemical Properties

Num. heavy atoms :	17
Num. arom. heavy atoms :	6
Fraction Csp3 :	0.46
Num. rotatable bonds :	5
Num. H-bond acceptors :	2.0
Num. H-bond donors :	1.0
Molar Refractivity :	72.46
TPSA :	38.33 Å²

Pharmacokinetics

GI absorption :	High
BBB permeant :	Yes
P-gp substrate :	No
CYP1A2 inhibitor :	No
CYP2C19 inhibitor :	Yes
CYP2C9 inhibitor :	Yes
CYP2D6 inhibitor :	No
CYP3A4 inhibitor :	No
Log Kp (skin permeation) :	-5.63 cm/s

Lipophilicity

Log Po/w (iLOGP) :	3.11
Log Po/w (XLOGP3) :	3.52
Log Po/w (WLOGP) :	3.71
Log Po/w (MLOGP) :	3.32
Log Po/w (SILICOS-IT) :	2.95
Consensus Log Po/w :	3.32

Druglikeness

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

Water Solubility

Log S (ESOL) :	-3.85
Solubility :	0.0424 mg/ml ; 0.000141 mol/l
Class :	Soluble
Log S (Ali) :	-4.01
Solubility :	0.0294 mg/ml ; 0.000098 mol/l
Class :	Moderately soluble
Log S (SILICOS-IT) :	-4.62
Solubility :	0.00712 mg/ml ; 0.0000237 mol/l
Class :	Moderately soluble

Medicinal Chemistry

PAINS :	0.0 alert
Brenk :	0.0 alert
Leadlikeness :	1.0
Synthetic accessibility :	2.53

Safety of [ 1187932-25-7 ]

Signal Word:	Warning	Class:	N/A
Precautionary Statements:	P280-P305+P351+P338	UN#:	N/A
Hazard Statements:	H302	Packing Group:	N/A
GHS Pictogram:

Application In Synthesis of [ 1187932-25-7 ]

* 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 [ 1187932-25-7 ]
Downstream synthetic route of [ 1187932-25-7 ]

[ 1187932-25-7 ] Synthesis Path-Upstream 1~1

1
[ 24424-99-5 ]
[ 176707-77-0 ]
[ 1187932-25-7 ]

Yield	Reaction Conditions	Operation in experiment
100%	With triethylamine In dichloromethane at 20℃;	Example 16, Compound 16; (E)-(2R,5S,11 S,14S,17R,18R)-11 -(3-Hydroxy-benzyl)-14-isopropyl-18-methoxy- 2,17-dimethyl-3,9,12,15,28-pentaaza-tricyclo[21.3.1.1 5,9]octacosa- 1 (27),21 ,23,25-tetraene-4,10,13,16-tetraone.; Com ound 16a: [(R)-1 -(3-Bromo-phenyl)-ethyl]-carbamic acid iert-butyl esterA solution of (R)-bromo-a-methylbenzylamine (1 .023 g, 5.1 12 mmol) indichloromethane (20 mL) was subsequently treated with triethylamine (720 μΙ_, 5.1 12 mmol) and di-te/t-butyl dicarbonate (1 .784 g, 8.179 mmol). After overnight stirring at room temperature, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of /so-hexanes/Et₂0 1 :0 to 4:1 to afford the title compound (1 .552 g, 100percent) as a white solid. H NMR (300 MHz, CDCI₃) 1 .43 (br s, 12H), 4.77 (br s, 2H), 7.16-7.26 (m, 2H), 7.39 (dt, J = 2.0, 7.1 Hz, 1 H), 7.46 (s, 1 H).
100%	With triethylamine In tetrahydrofuran at 20℃; for 3 h;	00198] To a solution of (R)-l-(3-bromophenyl)ethanamine (100 mg, 0.500 mmol) in tetrahydrofuran (4 mL) was added Et₃N (0.104 mL, 0.750 mmol), followed by di- tert-butyl dicarbonate (131 mg, 0.600 mmol). The reaction mixture was stirred at rt for 3 h. The solvent was removed under reduced pressure. The crude residue was diluted with Et₂0 and washed with IN HC1, H₂0 then dried over Na₂S0₄. The Et₂0 layer was concentrated in vacuum to give the crude Intermediate 33A (150 mg, 0.500 mmol, 100 percent yield). LC-MS (ESI) m/z 245.9 (M-Boc+H), RT = 2.13 min (Method
100%	With triethylamine In tetrahydrofuran at 20℃; for 3 h;	To a solution of (R)-l-(3-bromophenyl)ethanamine (0.10 g, 0.50 mmol) in tetrahydrofuran (4 mL) was added Et3 (0.10 mL, 0.75 mmol), followed by di-tert-butyl dicarbonate (0.13 g, 0.60 mmol). The reaction mixture was stirred at rt for 3 h. The solvent was removed under reduced pressure. The crude residue was diluted with Et₂0 and washed with 1 N HC1, H₂0 then dried over a₂S04. The Et₂0 layer was concentrated in vacuum to give the crude Intermediate 10A (150 mg, 0.500 mmol, 100percent yield). LC-MS (ESI) m/z 245.9 (M-Boc+H), RT = 2.13 min (Method B).

100%	With triethylamine In dichloromethane at 20℃;	Compound 1 h Synthesis of Compound 1h: A solution of (R)-bromo-a-methylbenzylamine (1.023 g, 5.1 12 mmol) in dichloromethane (20 ml.) was subsequently treated with triethylamine (720 μΙ_, 5.1 12 mmol) and di-ferf-butyl dicarbonate (1 .784 g, 8.179 mmol). After overnight stirring at room temperature, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of iso- hexane/diethyl ether 1 :0 to 4:1 to afford the title compound (1 .552 g, 100percent) as a white solid
100%	With triethylamine In dichloromethane at 20℃;	A solution of (R)-bromo-a-methylbenzylamine (1 .023 g, 5.1 12 mmol) in dichloromethane (20 mL) was subsequently treated with triethylamine (720 μ, 5.1 12 mmol) and di-ferf-butyl dicarbonate (1.784 g, 8.179 mmol). After overnight stirring at RT, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of /^'so-hexanes/diethyl ether 1 :0 to 4:1 to afford the title compound (1 .552 g, 100percent) as a white solid
100%	With triethylamine In dichloromethane at 20℃;	A solution of (R)-bromo-α-methylbenzylamine (1.023 g, 5.112 mmol) in dichloromethane (20 mL) was subsequently treated with triethylamine (720 μL, 5.112 mmol) and di-tert-butyl dicarbonate (1.784 g, 8.179 mmol). After overnight stirring at RT, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of iso-hexanes/ diethyl ether 1:0 to 4:1 to afford the title compound (1.552 g, 100percent) as a white solid.
84%	at 20℃; for 1 h;	Compound 6a Synthesis of Compound 6a: A solution of (R)-bromo-a-methylbenzylamine (2.0 g, 10 mmol) in dichloromethane (20 mL) was treated with a solution of di-ferf-butyl dicarbonate (2.4 g, 1 1 mmol) in dichloromethane (20 mL) and the reaction mixture was stirred at room temperature for 1 h. The solution was washed with 2 M hydrochloric acid, water and brine, dried over sodium sulfate, filtered and evaporated. The residue was purified by silica gel chromatography using a gradient of /^'so-hexane/ethyl acetate 20:1 to 6:1 to afford the title compound (2.51 g, 84percent) as a white solid.

Reference： [1] Patent: WO2012/78915, 2012, A1, . Location in patent: Page/Page column 90
[2] Patent: WO2013/48942, 2013, A1, . Location in patent: Paragraph 00198
[3] Patent: WO2013/151923, 2013, A1, . Location in patent: Paragraph 00186
[4] Patent: WO2013/185093, 2013, A1, . Location in patent: Page/Page column 61; 62
[5] Patent: WO2013/185103, 2013, A1, . Location in patent: Page/Page column 63
[6] Patent: US2017/190737, 2017, A1, . Location in patent: Paragraph 0206
[7] Patent: WO2013/185093, 2013, A1, . Location in patent: Page/Page column 76; 77
[8] Patent: WO2015/9977, 2015, A1, . Location in patent: Page/Page column 115

[ 1187932-25-7 ] Synthesis Path-Downstream 1~39

1
[ 1187932-25-7 ]
[ 7486-35-3 ]
[ 1381813-33-7 ]

Yield	Reaction Conditions	Operation in experiment
82%	bis-triphenylphosphine-palladium(II) chloride; In toluene; at 60℃; for 16h;Inert atmosphere;	Compound 16b: [(R)-1-(3-Vinyl-phenyl)-ethyl]-carbamic acid iert-butyl ester; A solution of [(R)-1 -(3-bromo-phenyl)-ethyl]-carbamic acid te/t-butyl ester (10.26 g, 0.0342 mol.) and tributyl(vinyl)stannane (32.5 g, 30ml_, 0.103 mol.) in toluene (175 mL) was purged with nitrogen for 30 minutes before addition of bis(triphenylphosphine palladium II chloride (2.38 g, 0.0034 mol.). The stirred mixture was heated to 60 C for 16 hours before cooling to room temperature. The reaction mixture was filtered through hyflo-supercel then evaporated to give a dark coloured oil. The oil was purified by silica gel chromatography using /so-hexanes/ethyl acetate 19:1 to yield the title compound (6.95 g, 82%) as a yellow oil. H NMR (300 MHz, CDCI3) deltalambda .39-1 .51 (m, 12H), 4.80 {br s, 2H), 5.24-5.32 (m, 1 H), 5.77 (d, J = 17.6 Hz, 1 H), 6.73 (dd, J = 17.6, 10.9 Hz, 1 H), 7.18-7.36 (m, 4H).
82%		Compound 1 i Synthesis of Compound 1i: A solution of 1 h (10.26 g, 0.0342 mol.) and tributyl(vinyl)stannane (32.5 g, 30ml_, 0.103 mol.) in toluene (175 mL) was purged with nitrogen for 30 minutes before addition of bis(triphenylphosphine palladium(ll) dichloride (2.38 g, 0.0034 mol). The stirred mixture was heated to 60 C for 16 h before cooling to room temperature. The reaction mixture was filtered through hyflo-supercel then evaporated to give a dark colored oil. The oil was purified by silica gel chromatography using /'so-hexane/ethyl acetate 19:1 to yield the title compound (6.95 g, 82%) as a yellow oil.
82%	With bis-triphenylphosphine-palladium(II) chloride; In toluene; at 60℃; for 16h;Inert atmosphere;	A solution of 1 g (10.26 g, 0.0342 mol.) and tributyl(vinyl)tin (32.5 g, 30 mL, 0.103 mol.) in toluene (175 mL) was purged with nitrogen for 30 min before addition of bis(triphenylphosphine) palladium (II) dichloride (2.38 g, 0.0034 mol.). The stirred mixture was heated to 60C for 16 h before cooling to RT. The reaction mixture was filtered through hyflo-supercel then evaporated to give a dark coloured oil. The oil was purified by silica gel chromatography using iso- hexanes/ethyl acetate 19:1 to yield the title compound (6.95 g, 82%) as a yellow oil

82%

With bis-triphenylphosphine-palladium(II) chloride; In toluene; at 60℃; for 16.5h;Inert atmosphere;

A solution of 1g (10.26 g, 0.0342 mol.) and tributyl(vinyl)tin (32.5 g, 30 mL, 0.103 mol.) in toluene (175 mL) was purged with nitrogen for 30 min before addition of bis(triphenylphosphine) palladium (II) dichloride (2.38 g, 0.0034 mol.). The stirred mixture was heated to 60 C. for 16 h before cooling to RT. The reaction mixture was filtered through hyflo-supercel then evaporated to give a dark coloured oil. The oil was purified by silica gel chromatography using iso-hexanes/ethyl acetate 19:1 to yield the title compound (6.95 g, 82%) as a yellow oil.

Reference： [1]Patent: WO2012/78915,2012,A1 .Location in patent: Page/Page column 90-91
[2]Patent: WO2013/185093,2013,A1 .Location in patent: Page/Page column 62
[3]Patent: WO2013/185103,2013,A1 .Location in patent: Page/Page column 63; 64
[4]Patent: US2017/190737,2017,A1 .Location in patent: Paragraph 0207

2
[ 24424-99-5 ]
[ 176707-77-0 ]
[ 1187932-25-7 ]

Yield	Reaction Conditions	Operation in experiment
100%	With triethylamine; In dichloromethane; at 20℃;	Example 16, Compound 16; (E)-(2R,5S,11 S,14S,17R,18R)-11 -(3-Hydroxy-benzyl)-14-isopropyl-18-methoxy- 2,17-dimethyl-3,9,12,15,28-pentaaza-tricyclo[21.3.1.1 5,9]octacosa- 1 (27),21 ,23,25-tetraene-4,10,13,16-tetraone.; Com ound 16a: [(R)-1 -(3-Bromo-phenyl)-ethyl]-carbamic acid iert-butyl esterA solution of (R)-bromo-a-methylbenzylamine (1 .023 g, 5.1 12 mmol) indichloromethane (20 mL) was subsequently treated with triethylamine (720 muIota_, 5.1 12 mmol) and di-te/t-butyl dicarbonate (1 .784 g, 8.179 mmol). After overnight stirring at room temperature, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of /so-hexanes/Et20 1 :0 to 4:1 to afford the title compound (1 .552 g, 100%) as a white solid. H NMR (300 MHz, CDCI3) 1 .43 (br s, 12H), 4.77 (br s, 2H), 7.16-7.26 (m, 2H), 7.39 (dt, J = 2.0, 7.1 Hz, 1 H), 7.46 (s, 1 H).
100%	With triethylamine; In tetrahydrofuran; at 20℃; for 3h;	00198] To a solution of (R)-l-(3-bromophenyl)ethanamine (100 mg, 0.500 mmol) in tetrahydrofuran (4 mL) was added Et3N (0.104 mL, 0.750 mmol), followed by di- tert-butyl dicarbonate (131 mg, 0.600 mmol). The reaction mixture was stirred at rt for 3 h. The solvent was removed under reduced pressure. The crude residue was diluted with Et20 and washed with IN HC1, H20 then dried over Na2S04. The Et20 layer was concentrated in vacuum to give the crude Intermediate 33A (150 mg, 0.500 mmol, 100 % yield). LC-MS (ESI) m/z 245.9 (M-Boc+H), RT = 2.13 min (Method
100%	With triethylamine; In tetrahydrofuran; at 20℃; for 3h;	To a solution of (R)-l-(3-bromophenyl)ethanamine (0.10 g, 0.50 mmol) in tetrahydrofuran (4 mL) was added Et3 (0.10 mL, 0.75 mmol), followed by di-tert-butyl dicarbonate (0.13 g, 0.60 mmol). The reaction mixture was stirred at rt for 3 h. The solvent was removed under reduced pressure. The crude residue was diluted with Et20 and washed with 1 N HC1, H20 then dried over a2S04. The Et20 layer was concentrated in vacuum to give the crude Intermediate 10A (150 mg, 0.500 mmol, 100% yield). LC-MS (ESI) m/z 245.9 (M-Boc+H), RT = 2.13 min (Method B).

100%	With triethylamine; In dichloromethane; at 20℃;	Compound 1 h Synthesis of Compound 1h: A solution of (R)-bromo-a-methylbenzylamine (1.023 g, 5.1 12 mmol) in dichloromethane (20 ml.) was subsequently treated with triethylamine (720 muIota_, 5.1 12 mmol) and di-ferf-butyl dicarbonate (1 .784 g, 8.179 mmol). After overnight stirring at room temperature, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of iso- hexane/diethyl ether 1 :0 to 4:1 to afford the title compound (1 .552 g, 100%) as a white solid
100%	With triethylamine; In dichloromethane; at 20℃;	A solution of (R)-bromo-a-methylbenzylamine (1 .023 g, 5.1 12 mmol) in dichloromethane (20 mL) was subsequently treated with triethylamine (720 mu, 5.1 12 mmol) and di-ferf-butyl dicarbonate (1.784 g, 8.179 mmol). After overnight stirring at RT, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of /'so-hexanes/diethyl ether 1 :0 to 4:1 to afford the title compound (1 .552 g, 100%) as a white solid
100%	With triethylamine; In dichloromethane; at 20℃;	A solution of (R)-bromo-alpha-methylbenzylamine (1.023 g, 5.112 mmol) in dichloromethane (20 mL) was subsequently treated with triethylamine (720 muL, 5.112 mmol) and di-tert-butyl dicarbonate (1.784 g, 8.179 mmol). After overnight stirring at RT, the volatiles were removed in vacuo and the residue was purified by silica gel chromatography using a 50 g Isolute cartridge eluted with a continuous gradient of iso-hexanes/ diethyl ether 1:0 to 4:1 to afford the title compound (1.552 g, 100%) as a white solid.
84%	In dichloromethane; at 20℃; for 1h;	Compound 6a Synthesis of Compound 6a: A solution of (R)-bromo-a-methylbenzylamine (2.0 g, 10 mmol) in dichloromethane (20 mL) was treated with a solution of di-ferf-butyl dicarbonate (2.4 g, 1 1 mmol) in dichloromethane (20 mL) and the reaction mixture was stirred at room temperature for 1 h. The solution was washed with 2 M hydrochloric acid, water and brine, dried over sodium sulfate, filtered and evaporated. The residue was purified by silica gel chromatography using a gradient of /'so-hexane/ethyl acetate 20:1 to 6:1 to afford the title compound (2.51 g, 84%) as a white solid.
	With N-ethyl-N,N-diisopropylamine; In dichloromethane; at 20℃;Inert atmosphere;	Boc-anhydride (3.71 ml, 16.0 mmol) was added to a solution of (R)-1-(3- bromophenyl)ethanamine (CAS 176707-77-0) (2.0 g, 10.0 mmol) and DIEA (1.83 ml, 10.5 mmol) in DCM (40.0 ml) at room temperature. After stirring overnight the reaction was purified directly by flash chromatography (100% DCM) to provide the title compound. 1H NMR (400 MHz, DMSO-c/6) delta ppm 7.49 (s, 1 H) 7.35 - 7.46 (m, 2 H) 7.20 - 7.35 (m, 2 H) 4.49 - 4.68 (m, 1 H) 1.18 - 1.49 (m, 12 H).

Reference： [1]Patent: WO2012/78915,2012,A1 .Location in patent: Page/Page column 90
[2]Patent: WO2013/48942,2013,A1 .Location in patent: Paragraph 00198
[3]Patent: WO2013/151923,2013,A1 .Location in patent: Paragraph 00186
[4]Patent: WO2013/185093,2013,A1 .Location in patent: Page/Page column 61; 62
[5]Patent: WO2013/185103,2013,A1 .Location in patent: Page/Page column 63
[6]Patent: US2017/190737,2017,A1 .Location in patent: Paragraph 0206
[7]Patent: WO2013/185093,2013,A1 .Location in patent: Page/Page column 76; 77
[8]Patent: WO2015/9977,2015,A1 .Location in patent: Page/Page column 115

3
[ 1187932-25-7 ]
[ 1381809-17-1 ]

Reference： [1]Patent: WO2012/78915,2012,A1

4
[ 1187932-25-7 ]
[ 1381813-39-3 ]

Reference： [1]Patent: WO2012/78915,2012,A1
[2]Patent: WO2013/185093,2013,A1
[3]Patent: WO2013/185103,2013,A1
[4]Patent: US2017/190737,2017,A1

5
[ 1187932-25-7 ]
[ 1381813-48-4 ]

Reference： [1]Patent: WO2012/78915,2012,A1

6
[ 1187932-25-7 ]
[ 1381813-63-3 ]

Reference： [1]Patent: WO2012/78915,2012,A1

7
[ 31166-44-6 ]
[ 1187932-25-7 ]
[ 865-48-5 ]
[ 1429187-90-5 ]

Yield	Reaction Conditions	Operation in experiment
96%	With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; In toluene; at 70℃; for 16h;	[00199] To a suspension of Intermediate 33 A (50 mg, 0.167 mmol) and Pd2(dba)3 (15.25 mg, 0.017 mmol) in toluene (2 mL) was added xantphos (28.9 mg, 0.050 mmol), benzyl piperazine-l-carboxylate (36.7 mg, 0.167 mmol), followed by sodium tert-butoxide (48.0 mg, 0.500 mmol). The reaction mixture was stirred at 70 C for 16 h, and then filtered. The filtrate was concentrated and purified on ISCO using a 15 min gradient from 0 to 100% EtOAc in hexane to give Intermediate 33B (70 mg,0.159 mmol, 96 % yield). LC-MS (ESI) m/z 440.1 (M+H), RT = 2.27 min (Method B).

Reference： [1]Patent: WO2013/48942,2013,A1 .Location in patent: Paragraph 00199

8
[ 1187932-25-7 ]
[ 1429187-89-2 ]

Reference： [1]Patent: WO2013/151923,2013,A1
[2]Patent: WO2013/48942,2013,A1

9
[ 1187932-25-7 ]
[ 1466528-31-3 ]

Reference： [1]Patent: WO2013/151923,2013,A1

10
[ 1187932-25-7 ]
(R)-1-(3-(1-phenethyl-1H-pyrazol-4-yl)phenyl)ethanamine hydrochloride [ No CAS ]

Reference： [1]Patent: WO2013/151923,2013,A1

11
[ 31166-44-6 ]
[ 1187932-25-7 ]
[ 1429187-90-5 ]

Yield	Reaction Conditions	Operation in experiment
96%	With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; sodium t-butanolate; In toluene; at 70℃; for 16h;	To a suspension of Intermediate 10A (50 mg, 0.17 mmol) and Pd2(dba)3 (15 mg, 0.017 mmol) in toluene (2 mL) was added Xantphos (29 mg, 0.050 mmol), benzyl piperazine-l-carboxylate (37 mg, 0.17 mmol), followed by sodium tert-butoxide (48 mg, 0.50 mmol). The reaction mixture was stirred at 70 C for 16 h, and then filtered. The filtrate was concentrated and purified by flash chromatography using a 15 min gradient from 0 to 100% EtOAc in hexanes to give Intermediate 10B (70 mg, 0.16 mmol, 96% yield). LC-MS (ESI) m/z 440.1 (M+H), RT = 2.27 min (Method B).

Reference： [1]Patent: WO2013/151923,2013,A1 .Location in patent: Paragraph 00187

12
[ 552846-17-0 ]
[ 1187932-25-7 ]
[ 1466528-30-2 ]