Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Water → (R)-5-[(1S,2S)-2-Amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2,2-diphenylmorpholine-4-carboxylic acid tert-butyl ester
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Water | HCID 962 | — |
| 반응물 | Sodium borohydride | HCID 4311764 | — |
| 반응물 | (R)-5-[(1R,2S)-3-(3,5-difluorophenyl)-1-hydroxy-2-nitropropyl]-2,2-diphenylmorpholine-4-carboxylic acid tert-butyl ester | HCID 68563474 | — |
| 촉매 | Nickel Dichloride | HCID 24385 | — |
| 용매 | Methanol | HCID 887 | — |
| 생성물 | (R)-5-[(1S,2S)-2-Amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2,2-diphenylmorpholine-4-carboxylic acid tert-butyl ester | HCID 68561345 | — |
반응 단계
Dissolve (R)-5-[(1R,2S)-3-(3,5-difluorophenyl)-1-hydroxy-2-nitropropyl]-2,2-diphenylmorpholine-4-carboxylic acid tert-butyl ester (0.172 g, 0.31 mmol) in dry methanol (8 mL), add nickel chloride (0.060 g, 0.46 mmol) then sodium borohydride (0.059 g, 1.55 mmol). Stir 15 minutes, add water (˜2 mL) and concentrate. Add ethyl acetate (˜70 mL), filter (Celite®), wash with water and saturated aqueous sodium chloride. Dry (magnesium sulfate), filter and concentrate to give the desired compound as a white solid.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07745438B2 |
| 출처 데이터셋 | uspto-grants-2010_06 |
| ORD ID | ord-3e2bffbbd863498888e852199d458adc |
| 출처 메모 | uspto-grants-2010_06 |