1-Hydroxybenzotriazole → 1-Butyl-N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl)-4-[methyl(methylsulfonyl)amino]-1H-indole-6-carboxamide

https://huagongshe.com/ko/reaction/14172

참여 물질

역할	이름	HCID	투입량
반응물	1-Hydroxybenzotriazole	HCID 75771	—
반응물	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
반응물	1-Butyl-4-[methyl(methylsulfonyl)amino]-1H-indole-6-carboxylic acid	HCID 21085174	—
반응물	(2R,3S)-3-amino-4-(3,5-difluorophenyl)-1-[(3-ethylbenzyl)amino]butan-2-ol	HCID 57487282	—
용매	Dichloromethane	HCID 6344	—
용매	Triethylamine	HCID 8471	—
생성물	1-Butyl-N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl)-4-[methyl(methylsulfonyl)amino]-1H-indole-6-carboxamide	HCID 57508185	53.2%

반응 조건

온도	40 °C

반응 단계

To a mixture of 1-Butyl-4-[methyl(methylsulfonyl)amino]-1H-indole-6-carboxylic acid (0.2 g) in methylene chloride (15 mL) was added triethylamine (0.156 g), HOBT (0.105 g), and HATU (0.293 g). The mixture was stirred at 39° C. for 10 minutes at which time (2R,3S)-3-amino-4-(3,5-difluorophenyl)-1-[(3-ethylbenzyl)amino]butan-2-ol (0.293 g) was added. The mixture was stirred at 40° C. for 4 h then poured into methylene chloride (50 mL), washed with water followed by brine then dried over anhydrous magnesium sulfate and concentrated under reduced pressure. Column chromatography on silica gel (100 mL) using 5% methanol in methylene chloride as eluent to give 0.21 g of the title compound: MS (ESI+) for C34H42F2N4O4S1 m/z 640.8 (M+H).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US07727997B2
출처 데이터셋	uspto-grants-2010_06
ORD ID	ord-34564fa2bde2476ea7d73a1bc60a19c3
출처 메모	uspto-grants-2010_06