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1. WO2000032585 - PROCESS FOR THE PREPARATION OF SIMVASTATIN AND ANALOGS THEREOF

Publication Number WO/2000/032585
Publication Date 08.06.2000
International Application No. PCT/IB1999/001912
International Filing Date 01.12.1999
Chapter 2 Demand Filed 20.06.2000
IPC
C07D 309/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
309Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
16having one double bond between ring members or between a ring member and a non-ring member
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
30Oxygen atoms, e.g. delta-lactones
CPC
C07D 309/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
309Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
16having one double bond between ring members or between a ring member and a non-ring member
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
30Oxygen atoms, e.g. delta-lactones
Applicants
  • LEK PHARMACEUTICAL AND CHEMICAL COMPANY D.D. [SI]/[SI] (AllExceptUS)
  • ŽLIČAR, Marco [SI]/[SI] (UsOnly)
Inventors
  • ŽLIČAR, Marco
Priority Data
P-980030002.12.1998SI
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF SIMVASTATIN AND ANALOGS THEREOF
(FR) PROCEDE DE PREPARATION DE SIMVASTATINE ET D'ANALOGUES DE CELLE-CI
Abstract
(EN)
Lovastatin, pravastatin, simvastatin, mevastatin, derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, and some are obtained by treating the fermentation products using the methods of chemical synthesis for example simvastatin. This invention relates to the novel method for the acylation of sterically hindered alcohols which is applicable in the process for the preparation of simvastatin and derivatives thereof.
(FR)
La lovastatine, la pravastative, la simvastatine, la mévastative et les dérivés et analogues de ces substances sont connus comme étant des inhibiteurs de HMG-CoA réductase et sont utilisés comme agent anti-hypercholestérolémique. La plupart de ces substances sont produites par fermentation à l'aide de micro-organismes d'espèces différentes identifiées comme des espèces appartenant au genre Aspergilus, Monascus, Nocardia, Amycolatopsis, Mucor ou Penicillium, et certaines de ces substances, comme la simvastatine, sont obtenues par traitement des produits de fermentation à l'aide de procédés de synthèse chimique. Cette invention se rapporte au nouveau procédé d'acylation d'alcools à empêchement stérique, qui est applicable dans le processus de préparation de la simvastatine et des dérivés de cette substance.
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