Richter Gedeon Vegyeszeti Gyar Rt

Marvishi Pharmaceutical Co., Ltd.

Richter Gedeon Nyrt.

Zoltan Tuba

Laszlo Szporny

Maria Marsai

Egon Karpati

Katalin Biro

Eva Palosi

Sandor Gorog

Bela Kiss

Ferenc Trischler

Szabolcs Szeberenyi

Aniko Gere

Pal Vittay

Antal Aranyi

Janos Brlik

Janos Szeles

Jozsef Bodi

Janos Csorgei

Judit Horvath

Bela Soros

Gyorgy Galik

Csaba Szantay

Maria Gazdag

Peter Horvath

Szaboles Szeberenyi

E Szilveszter Vizi

Adam Demeter

Maria Incze

Tamas Mester

Ferenc Soti

Krisztina Lancos

Francis F Foldes

Zsuzsa Baloghne Kardos

Anna M Boorne

Erzsebet C Francsicsne

Bela Sörös

Miklos Riesz, Deceased

Arpad Trompler

Gabriella Szilagyi

Erika Bakcsi

Katalin Ferenczi

Janos Horvath

Adam Bor

Laszle Szporny

György Galik

Maria Lovas Nee Marsai

Laszlo Terdy

Zoltan Horvath

Lajosne Dancsi

Endrene Magyari

A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.

Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide

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

There is disclosed novel, therapeutically active androstane derivatives having neuromuscular blocking effect, which are substituted by a quaternary ammonium group in 16-position; pharmaceutically composition containing them; process for producing them; and novel intermediates for the production.

Androstane derivatives substituted by a quaternary ammonium group in

Steroids with pregnane skeleton, pharmaceutical compositions containing

Biologically active eburnamenine derivatives, pharmaceutical

New monoquaternary and diquaternary 5-alpha-hydroxy-3,16-diaminoandrostane salts are disclosed with curare-like muscle relaxant activity. The new salts are characterized by a surprisingly rapid onset time.

Diamino-androstane derivatives

The invention relates to new 3-amino-17a-aza-D-homo-5.alpha.-androstane derivatives of the general formula I ##STR1## wherein R.sub.1 represents a methylene or an &gt;N--CH.sub.3 group, and n stands for 1 or 2, and the acid addition salts and the quaternary salts of the general formula ##STR2## thereof, wherein R.sub.2 stands for an alkyl or alkenyl group having from 1 to 4 carbon atoms, and A represents a halogen atom, provided that if R.sub.1 stands for an &gt;N--CH.sub.3 group, R.sub.2 is attached to the nitrogen of that &gt;N--CH.sub.3 group. The new compound possess a non-polarizing neuromuscular blocking activity and have a short activity period.

3-Amino-17a-aza-D-homoandrostane compounds, and pharmaceutical

Curare-type salts of the formula ##STR1## wherein Ac is an alkyl carbonyl group containing 1 to 4 carbon atoms in the alkyl moiety and one of

Diamino-androstanes and a process for the preparation of the said

5.alpha., 17B-Diacetoxy-6 -chloro-2.alpha., 3.alpha.; 16.alpha., 17.alpha.-diepoxy-androstane; 5.alpha., 17B-Dicetoxy-6 -chloro-androsta-2,16-diene; 5.alpha.-Hydroxy-6 -chloro-17-oxo-androst-2-ene or a like intermediate in the production of curare-like compounds is produced by reacting 5.alpha., 6B-dihydroxy-17-oxo-androst-2-ene with an organic sulfonic acid chloride. The obtained 5.alpha.- hydroxy-6B-chloro-17-oxo-androst-2-ene can then be reacted with the enol acetate of a ketone having 3 to 5 carbon atoms to yield 5.alpha., 17B-diacetoxy-6B-chloro-androsta-2,16-diene. The latter is treated to yield the corresponding diepoxide.

Diepoxy-androstanes and a process for the preparation thereof

A compound of the formula (I) ##STR1## wherein X is a halogen,

Acylated diepoxy-androstane and a process for the preparation thereof

Curare-type salts of the formula ##STR1## WHEREIN Ac is an alkyl carbonyl group containing 1 to 4 carbon atoms in the alkyl moiety and one of

New triamino-androstanes with curare-type properties and a process for the preparation thereof are disclosed.

Triamino-androstanes and a process for the preparation of the said

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Budapest, Hungary

Zoltan Tuba