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J Org Chem. 2017 Mar 17;82(6):2862-2869. doi: 10.1021/acs.joc.6b02761. Epub 2017 Mar 6.

A Diastereoselective Multicomponent Reaction for Construction of Alkynylamide-Substituted α,β-Diamino Acid Derivatives To Hunt Hits.

Author information

1
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Chemical Engineering, East China Normal University , 3663 North Zhongshan Road, Shanghai 200062, China.

Abstract

A highly diasetereoselective Mannich-type multicomponent reaction was developed to rapidly construct alkynylamide-substituted α,β-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.

PMID:
28225272
DOI:
10.1021/acs.joc.6b02761

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