期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 23, 期 3, 页码 554-557出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201605127
关键词
asymmetric catalysis; Lewis acid catalysis; sulfa-Michael reaction; synthesis design; alpha,beta-unsaturated pyrazolamide
资金
- National Natural Science Foundation of China [21432006, 21290182, 21321061]
- Top-Notch Young Talents program of China
An enantioselective sulfa-Michael-cyclization reaction was developed for the synthesis of 1,5-benzothiazepines with versatile pharmacological activities. The reaction between 2-aminothiophenol and alpha,beta-unsaturated pyrazoleamides gave direct access to N-H-free 1,5-benzothiazepines in the presence of a chiral N,N'-dioxide/Yb(OTf)(3) complex. Excellent enantioselectivities (up to 96% ee) and high yields (up to 99%) were obtained for a broad range of substrates under mild reaction conditions. This method provided a facile approach to the antidepressant drug (R)-(-)-Thiazesim.
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