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 Beckmann rearrangement. The absolute configuration was assigned by a Mosher's method.
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Xie et al. (2008) studied this question.
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