ML-236B Derivatives and their preparation
AssigneeSankyo Company, Limited
InventorsAkira Terahara, Minoru Tanaka
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongornella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.
Claims24
A process for preparing a compound of the formula (I). ##STR19## wherein R represents a group of formula ##STR20## or a ring-closed lactone, salt or ester thereof which comprises enzymatically hydroxylating a substrate selected from ML-236B having the formula ##STR21## or ML-236B carboxylic acid having the formula ##STR22## or a salt or ester of said ML-236B carboxylic acid with a microorganism of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces or with a cell-free, enzyme containing extract from said microorganisms to produce said compound of the formula (I), and recovering said compound of the formula (I).
A process is for preparing a compound having the formula (a):
- ##STR23## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group), pharmaceutically acceptable salts of the acid wherein R.sup.1 represents a hydrogen atom, and compounds of formula (b):
- ##STR24## by enzymatically hydroxylating a substrate selected from the group consisting of ML236B or ML236B carboxylic acid with a microorganism selected from the group consisting of Syncephalastrum nigricans and Syncephalastrum racemosum and recovering said compounds.
A process for preparing a compound having the formula (c):
- ##STR25## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group), pharmaceutically acceptable salts of the acid wherein R.sup.1 represents a hydrogen atom, and compounds of formula (d):
- ##STR26## by enzymatically hydroxylating a substrate selected from the group consisting of ML236B or ML236B carboxylic acid with a microorganism selected from the group consisting of Absidia coerulea and Cunninghamella echinulata and recovering said compounds.
Dependencies are inferred from the claim text.