Patent ID: 7700329
Filing Date: 2010-04-20
Classification: C07D,C12P

Abstract:
1. A method for the preparation of simvastatin comprising a homodiacylation process comprising: (a) enzymatic hydrolysis of lovastatin, lovastatin acid or a salt of lovastatin acid with an esterase enzyme to form a triol acid, wherein the esterase has a sequence having at least about 90% sequence identity to SEQ ID NO:2, SEQ ID NO:4 or SEQ ID NO:6; (b) forming a diol lactone from the triol acid by lactonization; (c) acylating the 4-position (4′-OH) and 8-position (8′-OH) on the lactone ring of the diol lactone by chemical acylation to form a 4,8-diacetyl lactone; and (d) removing selectively the acyl group at the 4′ position by enzymatic hydrolysis, thereby making simvastatin.