Ml-236b derivatives, a process for their preparation and pharmaceutical compositions containing them

Abstract From the Canadian patent

A compound of formula (1):, (I) (called 6-methoxy-IsoML-236B lactone) and its corresponding free hydroxy-carboxylic acid and salts and esters of said acid may be prepared by the enzymatic alkoxylation of an ML-236B compound preferably using a microorganism of the genus Syncephalastrum Absidia or Cunninghamella, e.g. Absidia coerulea or a cell-free, enzyme-containing extract from said microorganism. If desired the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester. These compounds have the ability to inhibit the biosynthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which …