C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 205/08 (2006.01) C07D 317/30 (2006.01) C07D 405/06 (2006.01) C07D 413/06 (2006.01) C07F 7/02 (2006.01)
Patent
CA 2630737
This invention provides a novel, industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)- [3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4- hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) wherein, the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, Rl, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert.buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group.
La présente invention concerne un nouveau procédé aisément réalisable industriellement et économique comprenant seulement quelques étapes, et basé sur de nouveaux intermédiaires pour la production de 1-(4-3(R)- [3(S)-(4-fluorophényl)-3-hydroxypropyl]-4(S)-(4-hydroxyphényl)-2-azétidinone (ézétimibe) conformément au schéma de réaction suivant : (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) où les substances de formules générales II, IV, VI, VIII, IX, X et XI sont nouvelles, la formule III est un intermédiaire non isolé, R1, R2 et R3 sont représentés par les composés de formules Va à Vd, (Va), (Vb), (Vc), (Vd) et R4 est un groupe silyle, par exemple, tert-butyl-diméthyl-silyle, tert-butyl-diphényl-silyle.
Bodi Jozsef
Eles Janos
Gati Tamas
Kiss-Bartos Dorottya
Szoke Katalin
Fetherstonhaugh & Co.
Richter Gedeon Nyrt.
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