Richter Gedeon Nyrt.

Richter Gedeon Vegyeszeti Gyar Rt

Csaba Sánta

Sándor Mahó

János Csörgei

Zoltán Béni

János Horváth

Janos Csorgei

Gábor Balogh

Zoltan Tuba

Antal Aranyi

Janos Szeles

Zoltan Beni

Janos Horvath

Ferenc Trischler

Gyorgy Visky

Zoltán Tuba

Peter Horvath

József Bódi

Adam Demeter

Csaba Molnar

László Terdy

Balazs Havasi

Janos Brlik

Tamas Mester

György Visky

Csaba Molnár

Gabriella Szilagyi

Erika Bakcsi

László Balogh

Tamás Schäfer

János Széles

Anita Horváth

Zoltán Horváth

Gábor Szabó

Attila Balázs

Katalin Ferenczi

Péter Vincze

Krisztina Lancos

Ádám Demeter

Arpad Trompler

Balázs Havasi

Jozsef Bodi

Laszlo Terdy

Zoltan Horvath

Anita Horvath

Gábor SzabÓ

The invention relates to the last step of a synthetic process, in which Nomegestrol-acetate of formula (I) is synthesized from 17&#x3b1;-acetoxy-6-methylene-19-norpregn-4-ene-3,20-dione of formula (II) in the presence of Pd/C catalyst and acetic acid in hot ethanolic solution. 

Industrial process for the synthesis of nomegestrol-acetate

The present invention relates to a process for the synthesis of compounds of formula (I), wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R' is dimethylamino or 2-methyl-1,3-dioxan-2-yl group, as starting material and methoxymethyl lithium as reagent. 

Process for the production of 21-methoxy-11-beta-phenyl-19-nor-pregna-4,9-diene-3,20-dione derivatives

The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process. 

Industrial process for the synthesis of ulipristal acetate and its 4'-acetyl analogue

The present invention relates to a new stereoselective process for the synthesis of 17(&#x3b1;)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(&#x3b1;)-17-acetyl-17-hydroxy-estr-4-en-3-one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activity&#x2014;such as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III). 

Process for the production of 19-norpregn-4-en-3,20-dione-17&#x3b1;-ol(gestonorone) and intermediates therefor

The present invention relates to novel crystalline Form II of 17&#x3b1;-acetoxy-21-methoxy-11&#x3b2;-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical compositions comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.

Crystal form of an organic compound and process for the preparation thereof

The present invention relates to novel crystalline Form A of 17&#x3b1;-acetoxy-21-methoxy-11&#x3b2;-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124) and methods for the preparation of it in excellent purity. 

Crystalline form of antiprogestin CDB-4124

The present invention relates to a process for the synthesis of the 17-acetoxy-11&#x3b2;-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II): 

Industrial method for the synthesis of 17-acetoxy-11&#x3b2;[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process

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

Csaba Sánta