Patent Number: 6,252,091

Title: Process for the preparation of simvastatin and derivatives thereof

Abstract: A process for the preparation of compounds of formula (I) ##STR1## wherein R is a C.sub.1 to C.sub.12 alkyl group and R.sub.1 is a protecting group or H which process comprises (a) converting the diol lactone of formula (II) ##STR2## to the protected diol lactone of formula (IIa) wherein R.sub.1 is a protecting group ##STR3## (b) acylating the protected diol lactone (IIa) to give compound (I) wherein R.sub.1 is a protecting group, (c) optionally removing the protecting group R.sub.1 to give compound (I) wherein R.sub.1 is H; and wherein steps (a) and/or (b) are carried out in the presence of N-methylimidazole.

Inventors: Zupancic ; Silvo (Novo mesto, SI), Stimac; Anton (Ljubljana, SI), Gnidovec; Joze (Novo mesto, SI)

Assignee: KRKA, Tovarna Zdravil, D.D.

International Classification: C07D 309/00 (20060101); C07D 309/30 (20060101); C07D 309/30 ()

Expiration Date: 06/26/2018