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1. WO2007144780 - PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF

Publication Number WO/2007/144780
Publication Date 21.12.2007
International Application No. PCT/IB2007/002885
International Filing Date 29.03.2007
IPC
C07D 205/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
06having one double bond between ring members or between a ring member and a non-ring member
08with one oxygen atom directly attached in position 2, e.g. beta-lactams
CPC
C07D 205/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
06having one double bond between ring members or between a ring member and a non-ring member
08with one oxygen atom directly attached in position 2, e.g. beta-lactams
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of products other than chlorine, adipic acid, caprolactam, or chlorodifluoromethane, e.g. bulk or fine chemicals or pharmaceuticals
55Synthetic design, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • Medichem S.A. [ES]/[ES] (AllExceptUS)
  • ESCUDÉ, Ana Gavaldá i [ES]/[ES] (UsOnly)
  • LLADÓ, Jordi Bosch i [ES]/[ES] (UsOnly)
  • NETTEKOVEN, Ulrike [CH]/[CH] (UsOnly)
Inventors
  • ESCUDÉ, Ana Gavaldá i
  • LLADÓ, Jordi Bosch i
  • NETTEKOVEN, Ulrike
Agents
  • VAN BUSKIRK, Tedd
Priority Data
60/786,72029.03.2006US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF
(FR) PROCÉDÉS DE SYNTHÈSE D'ÉZÉTIMIBE ET COMPOSÉS INTERMÉDIAIRES POUVANT ÊTRE EMPLOYÉS DANS SA SYNTHÈSE
Abstract
(EN)
The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.
(FR)
La présente invention concerne de façon générale un procédé amélioré de conversion de composés de Formule (II) (ci-dessous) en composés de Formule (III) (ci-dessous), qui sont des intermédiaires clés dans la synthèse de l'ézétimibe, ou l'ézétimibe lui-même, où dans les Formules (II) et (III), R représente un atome d'hydrogène ou un groupement alkyle ou protecteur de groupement hydroxy (par exemple benzyle, benzyle substitué ou silyle). La présente invention concerne également l'emploi du procédé décrit et l'emploi des composés de Formule (III) fabriqués à l'aide du procédé décrit dans la synthèse de l'ézétimibe.
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