申请人:Mitsubishi Tanabe Pharma Corporation
公开号:US08084611B2
公开(公告)日:2011-12-27
The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.
Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
本发明提供了一种制备光学活性四氢喹啉衍生物的方法,该方法可用于治疗和/或预防动脉硬化性疾病、血脂异常等疾病,以及制备其合成中间体的方法。具体而言,本发明通过较少的步骤而不使用光学分辨法,制备了(2R,4S)-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐,并从胺化合物中获得了光学活性四氢喹啉衍生物。