Richter Gedeon Nyrt.

Katalin Szöke

János Éles

Ferenc Faigl

József Bódi

Krisztina Vukics

János Fischer

Tamás Gáti

Krisztina Temesvári

Dorottya Kiss-Bartos

Ferencné Kassai

Béla Mátravölgyi

Viktor UJVÁRI

Zoltán NÉMET

Róbert Kiss

János FaragÓ

József Schindler

Attila Szemzö

Andrea Donát

Péter Erdelyi

A process 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) where the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silyl, e.g., tert-butyl-dimethyl-silyl, tert-butyl-diphenyl-silyl group. 

Process for the production of ezetimibe and intermediates used in this process

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Budapest, Hungary

Katalin Szöke