Alpha-hydroxy-beta-aminothiolcarboxylic esters and method and intermediates for their production

摘要

A method for producing alpha -hydroxy- beta -aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from alpha -amino acids. Starting from an N-protected alpha -amino acid ester, this is converted into a beta -ketosulfoxide, which is then reacted with an acid to give an alpha -keto-hemimercaptal. This is acylated and then processed with a base to obtain an N-protected alpha -acyloxy- beta -amino-thioester, which is then saponified to obtain the intended compound.