INTERMEDIATE OF CILASTATIN AND PREPARATION METHOD THEREOF

摘要

Disclosed is a method for preparing 7-halo-2-oxo-heptylate, an intermediate of cilastatin. The main steps are as follows: A. Addition reaction, in which 6-halo-hexanal is reacted with a cyanide to obtain 7-halo-a-hydroxyl-heptonitril; B. Hydrolysis reaction, in which 7-halo-a-hydroxyl- heptonitril is converted into 7-halo-a-hydroxyl-heptylic acid; C. Esterification reaction, in which 7-halo-a-hydroxyl-heptylic acid is converted into 7-halo-a-hydroxyl-heptylate, and D. Oxidation reaction, in which 7-halo-a-hydroxyl-heptylate is converted into 7-halo-2-oxo-heptylate.7-halo-a-hydroxyl-heptylic acid or ester, which is a new intermediate for synthesizing 7-halo-2-oxo-heptylate or cilastatin, and a method for synthesizing cilastatin are also disclosed. The methods of the invention are suitable for commercial production because of their simple process and mild reaction condition.