CIAT with simultaneous epimerization at two stereocenters. Synthesis of substituted beta-methyl-alpha-homophenylalanines

Org Biomol Chem. 2007 Jan 7;5(1):121-4. doi: 10.1039/b613103d. Epub 2006 Nov 23.

Abstract

Diastereoselective aza-Michael additions of phenylethylamine to 3-aroylbutenoic acids are reported. During these processes, efficient control over two new stereogenic centers on the Michael acceptor has been possible via crystallization-induced asymmetric transformation (CIAT). As an application, a convenient two-step synthesis of anti-beta-methylhomophenylalanines is also described.