FOERFARANDE FOER FRAMSTAELLNING AV NYA N N -DIACYLHYDRAZINDERIVAT FOER FOERHINDRANDE AV TUBERKULOS

摘要

1323170 N,N1-Diacylhydrazine derivatives RICHTER GEDEON VEGYESZETI GYAR RT 23 Dec 1970 [29 Dec 1969] 61178/70 Heading C2C The invention comprises N,N1-diacylhydrazine derivatives of the Formula I wherein X is H or a carboxylic acyl radical, R is H or a substituted or unsubstituted alkyl, aryl or aralkyl group, and Ac is the acyl radical of a substituted or unsubstituted aliphatic, aromatic or heterocyclic carboxylic acid and the pharmaceutically acceptable acid addition salts of those compounds containing a sufficiently basic nitrogen atom, and the optically active isomers of such compounds containing an asymmetric carbon atom. The compounds are prepared by (a) reactingα-aminoxy carboxylic acid derivatives of the Formula II wherein A is a carboxylic acyl radical, or when an end product X is H, A is a radical which protects the amino group, and B is OH or reactive functional derivative thereof, with hydrazides of the Formula III or (b) reactingα-aminoxy carboxylic acid hydrides of the Formula IV with carboxylic acids or reactive functional derivatives thereof of the Formula V and optionally converting the resulting compounds of the Formula VI obtained by either of the reactions mentioned above, into compounds of Formula I by removing the protective group A, and, if desired, acylating the resulting free amino group. Pharmaceutical compositions, suitable for oral, parenteral or rectal administration, contain the above novel compounds or acid addition salts thereof and suitable excipients or carriers. The compounds possess tuberculostatic activity.