Richter Gedeon Vegyeszeti Gyar Rt

Tamas Mester

Csaba Szantay

Bela Stefko

Janos Kreidl

Gabor Blasko

Erik Bogsch

Andras Nemes

Istvan Hegedus

Andras Vedres

Denes Mathe

Zoltan Tuba

Peter Horvath

Janos Szeles

Arpad Trompler

Krisztina Lancos

Adrien Szuchovszky, Nee Gergely

Katalin Ferenczi

Adrien Szuchovszky Nee Gergely

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

The invention relates to a new process for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine of the formula (I), ##STR1## which comprises reacting a pyrimidine derivative of the general formula (II), ##STR2## wherein R.sub.1 stantds for hydrogen or a ##STR3## group, wherein R means a C.sub.1-6 alkyl group or an aryl group optionally substituted by halogen;

Preparation of

A pyrimidine derivative of the formulae (Ia), (Ib) and (Ic), ##STR1## wherein R stands for an alkyl group group with 1 to 6 carbon atoms or an aryl group optionally substituted by halogen atom; and

Pyrimidine derivatives and process preparing the same

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Budapest, Hungary

Tamas Mester