Richter Gedeon Vegyeszeti Gyar Rt

Janos Szeles

Sándor Mahó

Zoltan Tuba

Csaba Sánta

Ferenc Trischler

Gábor Balogh

Gyorgy Visky

Peter Horvath

Antal Aranyi

Janos Brlik

Tamas Mester

Csaba Molnar

Katalin Ferenczi

Krisztina Lancos

Arpad Trompler

Gabriella Szilagyi

Erika Bakcsi

Jozsef Bodi

Janos Csorgei

Laszlo Terdy

Zoltan Horvath

The invention relates to a new process for the synthesis of 17&bgr;-hydroxy-17&agr;-methyl-2-oxa-5&agr;-androstane-3-one of formula (I). The process according to the invention is as follows: the 17&bgr;-hydroxy-17&agr;-ethyl-1,3-seco-2-nor-5&agr;-androstane-1,3-diacid of formula (III) is transformed into the ring-closed 17&bgr;-hydroxy-17&agr;-methyl-1,3-seco-2-nor-5&agr;-androstane-1,3-diacid anhydride of formula (II) in an inert solvent or without solvent with a C -C alkan acid anhydride or a substituted carbodiimide of formula R &mdash;N&boxH;C&boxH;N&mdash;R &mdash; wherein R and R independently are C -C alkyl group, C -C alkyl group substituted by tertiary or quaternary amino group or 1-3 phenyl group, C -C cycloalkyl group, aryl group substituted by 1-3 methoxy, tertiary amino, nitro, C -C alkyl group or 1-3 halogen atom&mdash;and the obtained compound of formula (II) is reduced regioselectively by a complex alkali metal hydride in an inert solvent The new 17&bgr;-hydroxy-17&agr;-methyl-1,3-seco-2-nor-5&agr;-androstane-1,3-diacid anhydride of formula (II) is also the subject of the invention.

Process for the synthesis of 17&bgr;-hydroxy-17&agr;-methyl-2-oxa-5&agr;-androstane-3-one

Process for the synthesis of a-nor-seco compounds with sterane skeleton

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Budapest, Hungary

Janos Szeles