METHOD FOR THE PREPARATION OF N-FORMYL-(S)-ISOSERINE

摘要

The invention relates to method for the preparation of a compound which is formyl derivative of the non-natural amino acid (S)-2-hydroxy-3-aminopropionic acid, used as acylating means. By the method high yield is produced of crystal product N-formyl-(S)-isoserine by the formylation of (S)-isoserine in a medium of acetonitrile and formic acid at room temperature at continuous agitation with 1.5-3 mol/mol 2-formylmercaptobenzothiazole, preferably 2.5 mol/mol. After the termination of the formylation process, the reaction mixture is cooled with icy water and the separated 2-mercaptobenzothiazole is filtered, and the excess of 2-formylmercaptobenzothiazole are filtered. The sludge is washed with acetonitrilke, the filtrate produced is concentrated to 1/4 of its initial volume, and the separated sludge us filtered again. The filtrate is purified by boiling in an influx and crystallization occurs during cooling, twice from ethyhlacetate and twice from acetone. The produced N-formyl-(S)-isoserine crystals mare filtered, washed in cooled acetone and are dried at room temperature. 2 claims