公开(公告)号：DE2940443A1

公开(公告)日：1981-04-16

申请号：DE2940443

申请日：1979-10-05

Applicant: BASF AG

Inventor： HICKMANN ECKHARD DIPL CHEM DR ,  OESER HEINZ-GUENTER DIPL CHEM ,  MOEBIUS LEANDER DIPL CHEM DR

IPC: C07D401/06 ,  A61K31/47 ,  C07D209/38 ,  C07D211/22 ,  C07D215/14 ,  C07D215/50

Abstract: 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.