期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 77, 期 6, 页码 2947-2953出版社
AMER CHEMICAL SOC
DOI: 10.1021/jo2025288
关键词
-
资金
- National Natural Science Foundation of China [20802075, 21042006]
A highly diastereoselective and enantioselective Michael addition of alpha-substituted isocyanoacetates with maleimides catalyzed by bifunctional tertiary amine thioureas has been developed. Various chiral succinimide derivatives bearing adjacent quaternary and tertiary stereocenters were prepared in excellent yields (up to 98%), diastereoselectivities (up to 99:1), and enantioselectivities (up to 98% ee). The synthetic utility of chiral succinimide derivatives is also demonstrated in the preparation of h5-HT1d receptor agonist motifs.
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