An aza-Michael addition protocol to fluoroalkylated β-amino acid derivatives and enantiopure trifluoromethylated N-heterocycles

Literature Information

Publication Date 2014-08-15
DOI 10.1039/C4GC01357C
Impact Factor 10.182
Authors

Xing Yang, Zhuo Chen, Yuan Cai, Yi-Yong Huang, Norio Shibata


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Abstract

The aza-Michael reaction with β-fluoroalkylated acrylates provided the corresponding fluoroalkylated β-amino acid derivatives in up to 99% yield under catalyst- and solvent-free conditions. An enantioenriched β-trifluoromethylated β-amino acid was obtained in good yield through a scale-up diastereoselective aza-Michael addition, which facilitated the installation of enantiopure trifluoromethylated analogues of β-lactam and dihydroquinolin-4-one.

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