A Diastereoselective Multicomponent Reaction for Construction of Alkynylamide-Substituted alpha,beta-Diamino Acid Derivatives To Hunt Hits

作者：Lei, Ruirui; Wu, Yong; Dong, Suzhen; Jia, Kaili; Liu, Shunying^*; Hu, Wenhao^*

来源：Journal of Organic Chemistry, 2017, 82(6): 2862-2869.

DOI：10.1021/acs.joc.6b02761

• Anticancer activities
• BEL-7402
• Diamino acids
• Diastereoselective
• Mannich
• Multi-component reactions

A highly diasetereoselective Mannich-type multicomponent reaction was developed to rapidly construct alkynylamide-substituted alpha,beta-diamino acid derivatives from simple starting materials under mild conditions in moderate to good yields for hit hunting. Most of the resulting products 4 exhibited good anticancer activity in HCT116, BEL7402, and SMMC7721 cells.

• 出版日期2017-3-17
• 单位华东师范大学