ES253914A1 - 2, 4-diaminoquinazolines and their preparation - Google Patents

Abstract

The invention comprises the following 2,4-diamino-R-quinazolines where R is 5,6-trimethylene, 5-methyl, 6-n-propyl, 6-n-butyl, 5,6-tetramethyl and 5-ethyl and the preparation of 2,4-diaminoquinazolines of the general formula <FORM:0935381/IV(a)/1> wherein R1 is a lower alkyl group and R2 is a hydrogen atom or a lower alkyl group and R1 may be a hydrogen atom when R2 is a lower alkyl group, R1 and R2 together having not more than 10 carbon atoms, or R1 and R2 together form an alkylene chain having 3 or 4 carbon atoms, by reacting an anthranilonitrile of the formula <FORM:0935381/IV(a)/2> with dicyandiamide, and pharmaceutical compositions containing the specified 2,4-diamino-R-quinazolines (see Group VI). 2-Amino-5-ethylebenzonitrile is prepared by decomposition of 5-ethylisatin b -oxime. Similarly are prepared 2-amino-6-methyl-benzonitrile, 2-amino-5-n-propylbenzonitrile, 2-amino-5-n-butylbenzonitrile, 2-amino-5,6,7, 8-tetrahydro-1-naphthonitrile and 2-amino-6-ethylbenzonitrile. 5-Amino-4-cyanoindane is prepared by reacting 5-acetylamino-4-bromoindane with cuprous cyanide to give 5-acetylamino-4-cyano-indane and removing the acetyl group by hydrolysis.ALSO:Antibacterial compositions contain 2,4-diamino-R-quinazolines, wherein R is 5,6-trimethylene, 5-methyl, 6-n-propyl, 6-n-butyl, 5,6-tetramethyl and 5-ethyl, together with a pharmaceutically acceptable carrier. The compositions may also contain antibiotics and/or antibacterials. The compositions may be presented as capsules or cachets containing fine powders or granules of the compounds in the dry state or in a non-aqueous suspension, in tablets, dragees, as solutions, suspensions or emulsions for oral administration as aqueous solutions for injection as suppositories or pessaries as ointments, creams or solutions for topical use.