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5-Bromo-2-chloropyrimidine → (-)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-7,7-dimethyl-2-[1-(5-methylthiopyrimidin-2-yl)-piperidin-4-yl]-5,6,7,8-tetrahydroquinolin-5-ol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-Bromo-2-chloropyrimidine | HCID 606665 | — |
| 反応物 | 2-Chloro-5-(methylthio)pyrimidine | HCID 21979532 | — |
| 反応物 | (-)-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 | — |
| 生成物 | (-)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-7,7-dimethyl-2-[1-(5-methylthiopyrimidin-2-yl)-piperidin-4-yl]-5,6,7,8-tetrahydroquinolin-5-ol | HCID 86682467 | — |
反応手順
Reactions similar to those of the first step of Example 2 and Example 38 were performed except for using 2-chloro-5-methylthiopyrimidine, which was prepared by a method similar to that of Reference Example 36, instead of 5-bromo-2-chloropyrimidine, and from 60 mg (89 μmol) 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, 50 mg of the title compound was obtained as a white solid (yield: 84%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09187450B2 |
| 出典データセット | uspto-grants-2015_11 |
| ORD ID | ord-6db5f363b45942189ed9a85bb781393b |
| 出典メモ | uspto-grants-2015_11 |