Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
5-Bromo-2-chloropyrimidine → (-)-2-[1-(5-Cyanopyrimidine-2-yl)piperidin-4-yl]-4-(4,4-difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-7,7-dimethyl-5,6,7,8-tetrahydroquinoline-5-ol
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | 5-Bromo-2-chloropyrimidine | HCID 606665 | — |
| 반응물 | 2-Chloro-5-pyrimidinecarbonitrile | HCID 21473592 | — |
| 반응물 | (-)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-5-[(4-methoxybenzyl)oxy]-7,7-dimethyl-2-(piperidin-4-yl)-5,6,7,8-tetrahydroquinoline | HCID 86682426 | — |
| 생성물 | (-)-2-[1-(5-Cyanopyrimidine-2-yl)piperidin-4-yl]-4-(4,4-difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-7,7-dimethyl-5,6,7,8-tetrahydroquinoline-5-ol | HCID 76372415 | — |
반응 단계
Reactions similar to those of the first step of Example 2 and Example 38 were performed except for using 2-chloropyrimidine-5-carbonitrile, which was synthesized by the method described in A. Takamizawa et al., Journal of Organic Chemistry, 1964, Vol. 29, pp. 1740-1742, instead of 5-bromo-2-chloropyrimidine, and from 78 mg (0.12 mmol) of (−)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-5-[(4-methoxybenzyl)oxy]-7,7-dimethyl-2-(piperidin-4-yl)-5,6,7,8-tetrahydroquinoline, which was prepared by a method similar to that of Reference Example 10, 60 mg of the title compound was obtained as a white solid (yield: 79%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US09187450B2 |
| 출처 데이터셋 | uspto-grants-2015_11 |
| ORD ID | ord-918116f058844acf924e2901b7b36fea |
| 출처 메모 | uspto-grants-2015_11 |