期刊
ORGANIC LETTERS
卷 13, 期 12, 页码 3118-3121出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol2010193
关键词
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资金
- Duke University
- Duke University, NCRR/NIH [1 UL1 RR024128-01]
- NCBC [2008-IDG-1010]
Mefloquine hydrochloride is an important antimalarial drug. It is currently manufactured and administered in racemic form; however there are indications regarding the biological activity of the two enantiomers that suggest the superiority of the (+)-form. The asymmetric total synthesis of the (+)-enantiomer of mefloquine hydrochloride is described. The key asymmetric transformation utilized is a novel asymmetric Darzens reaction of a chiral alpha-chloro-N-amino cyclic carbamate hydrazone derived from an N-amino cyclic carbamate (ACC) chiral auxiliary.
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