Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
(R)-3-(tert-butoxycarbonylamino)-4-(2,4,5-trifluorophenyl)butanoic acid → [7-[(3R)-3-[(tert-Butoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-alpha]pyrazin-8-yl](cyclopropyl)methanol
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | (R)-3-(tert-butoxycarbonylamino)-4-(2,4,5-trifluorophenyl)butanoic acid | HCID 7146288 | — |
| 반응물 | [2-(Trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-alpha]pyrazin-8-yl](cyclopropyl)methanol hydrochloride | HCID 69363534 | — |
| 생성물 | [7-[(3R)-3-[(tert-Butoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-alpha]pyrazin-8-yl](cyclopropyl)methanol | HCID 87798384 | — |
반응 단계
A 160 mg portion of [2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-α]pyrazin-8-yl](cyclopropyl)methanol hydrochloride was coupled to (3R)-3-[(tert-butoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid essentially following the procedure outlined in Example 2, Step D. Purification by preparative TCL (silica gel, 10% methanol/dichloromethane) gave 176 mg of the product as a mixture of diastereomers. HPLC (OD chiralcel column, 6% ethanol/hexane) separated the first and last eluting diastereomers. The middle fractions containing two diastereomers were further subjected to HPLC (OD chiralcel column, 3% ethanol/hexane) to provide the second and the third eluting diastereomers.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07390809B2 |
| 출처 데이터셋 | uspto-grants-2008_06 |
| ORD ID | ord-dc4e295dc3844936933b570d5dc2a19e |
| 출처 메모 | uspto-grants-2008_06 |