| 摘要 |
The present invention relates to a simplified process, which avoids organo-lithium intermediates, for the preparation of erythro- alpha -piperid-2-yl-2,8-bis-(trifluoromethyl)-quinolin-4-yl-methanol, wherein 2,8-bis-(trifluoromethyl)-quinoline-4-carboxylic acid or a salt thereof is reacted with a pyrid-2-yl-magnesium halide to give pyrid-2-yl-2,8-bis-(trifluoromethyl)-quinolin-4-yl ketone in the manner of a Grignard reaction, and this product is hydrogenated, in a conventional manner, to give erythro- alpha -piperid-2-yl-2,8-bis-(trifluoromethyl)-quinolin-4-yl-methanol. |
