돌아가기
Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 20429생성일: 2026년 10월 24일

Cesium carbonate → (2R,5R)-5-{(1S,2S)-2-Acetylamino-3-[3-(2,2-difluoroethoxy)-phenyl]-1-hydroxypropyl}-2-(1-methylcyclopentylmethoxy)-morpholine-4-carboxylic acid tert-butyl ester

https://huagongshe.com/ko/reaction/20429

반응식

참여 물질

역할이름HCID투입량
반응물Cesium carbonateHCID 10796—
반응물2-Bromo-1,1-difluoroethaneHCID 136186—
반응물(2R,5R)-5-[(1S,2S)-2-Acetylamino-1-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(1-methylcyclopentylmethoxy)-morpholine-4-carboxylic acid tert-butyl esterHCID 68562669—
용매DimethylformamideHCID 6228—
용매Ethyl AcetateHCID 8857—
생성물(2R,5R)-5-{(1S,2S)-2-Acetylamino-3-[3-(2,2-difluoroethoxy)-phenyl]-1-hydroxypropyl}-2-(1-methylcyclopentylmethoxy)-morpholine-4-carboxylic acid tert-butyl esterHCID 58972247—

반응 조건

온도60 °C

반응 단계

Dissolve (2R,5R)-5-[(1S,2S)-2-acetylamino-1-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(1-methylcyclopentylmethoxy)-morpholine-4-carboxylic acid tert-butyl ester (204 mg) and 2,2-difluoro-1-bromoethane (0.065 mL) and cesium carbonate (391 mg) in N,N-dimethylformamide (5 mL) and heat to 60° C. for 18 hours. Dilute with ethyl acetate, wash with saturated aqueous sodium chloride, dry and purify (silica gel chromatography, eluting with 1:1 ethyl acetate:dichloromethane), to give the desired compound (223 mg).

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US07745438B2
출처 데이터셋uspto-grants-2010_06
ORD IDord-50f5559b755c41c4bb23b87a638117e2
출처 메모uspto-grants-2010_06