Asymmetric Synthesis of (+)-(11 R,12S)-Mefloquine Hydrochloride

• 来源期刊: 中国化学（英文版）
• 年，卷（期）: 2008,（7）
• 页码范围: 1272-1276
• 页数: 5页
• 语种: 英文

摘要

The asymmetric synthesis of (+)-(11R,12S)-mefloquine hydrochloride, an antimalarial drug, was accomplished from commercially available 2-trifluoromethylaniline, ethyl 4,4,4-trifluoroacetoacetate and cyclopentanone in 7 steps with a 14% overall yield. The key steps were proline-catalyzed asymmetric direct aldol reaction and Beck-mann rearrangement. The absolute configuration was assigned by a Mosher's method.