| 摘要 |
The present invention provides a simple and inexpensive method for producing alpha -hydroxy- beta -aminocarboxylic acids and their esters. An ester of an N-protected alpha -amino acid ester is converted into a beta -ketosulfoxide, which is then processed with an acid to give an alpha -ketohemimercaptal. Next, 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 an intended compound. According to the method of the present invention, it is possible to produce alpha -hydroxy- beta -aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.
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