Richter Gedeon Vegyeszeti Gyar Rt

Maria Marsai

Zoltan Tuba

Laszlo Szporny

Egon Karpati

Katalin Biro

Szabolcs Szeberenyi

Sandor Gorog

Szaboles Szeberenyi

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.

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Budapest, Hungary

Maria Marsai