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HRID 715887作成日:2026年10月25日

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

https://huagongshe.com/reaction/715887

反応式

関与物質

役割名称HCID仕込み量
反応物5-Bromo-2-chloropyrimidineHCID 606665—
反応物2-Chloro-5-(methylthio)pyrimidineHCID 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-tetrahydroquinolineHCID 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-olHCID 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

DOI10.6084/m9.figshare.5104873.v1
特許番号US09187450B2
出典データセットuspto-grants-2015_11
ORD IDord-6db5f363b45942189ed9a85bb781393b
出典メモuspto-grants-2015_11