PROCESS FOR PREPARATION OF OPTICALLY ACTIVE AMINOLACTONE DERIVATIVES AND INTERMEDIATES OF THE DERIVATIVES

摘要

Optically active aminobutyric acid derivatives can be efficiently prepared, which are important intermediates of interleukin-1 beta -converting enzyme inhibitors. An optically active imine (1) is prepared by condensation of an optically active amine (6) with a dialkoxyaldehyde through dehydration, and then converted into an optically active aminobutyric acid derivative (3) through stereoselective addition; and the derivative (3) is further converted into an optically active aminolactone derivative (8) through stereoselective lactonization with an acid. (6) (1) (3) (8)