3-Fluoro-4-methylaniline → (RS)-4-(tert-Butyl-dimethyl-silanyloxy)-1-(3-fluoro-4-methyl-phenylamino)-butan-2-ol

참여 물질

역할	이름	HCID	투입량
반응물	3-Fluoro-4-methylaniline	HCID 9957	—
반응물	(R)-tert-butyldimethyl(2-(oxiran-2-yl)ethoxy)silane	HCID 11030897	—
용매	Acetonitrile	HCID 6342	—
생성물	(RS)-4-(tert-Butyl-dimethyl-silanyloxy)-1-(3-fluoro-4-methyl-phenylamino)-butan-2-ol	HCID 66954684	94.3%

반응 조건

온도	50 °C

반응 단계

LiClO4 (6.31 g, 60 mmol) was added to a solution of (RS)-tert-butyl-dimethyl-(2-oxiranyl-ethoxy)-silane (4 g, 20 mmol, prepared according to Heterocycles (1987), 25(1), 329-32) in MeCN (60 mL). 3-Fluoro-4-methylaniline (2.28 g, 18 mmol) was added and the mixture was stirred at 50° C. for 5 h. The solvent was removed under reduced pressure and the residue was purified by CC (DCM/MeOH/NH4OH 1000:25:2) to afford the title intermediate as brown oil (5.56 g, 86%).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08217029B2
출처 데이터셋	uspto-grants-2012_07
ORD ID	ord-af679ec97c2d4bd9942597c02c944a7e
출처 메모	uspto-grants-2012_07