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Abstract

Novel benzologs or pyrazolo-quinazoline derivatives of the formula (I) ##STR1## wherein X and Y are independently selected from oxygen, sulphur and imino and wherein ring (C) is a pyrazole ring fused to ring (B) via one of the three ortho positions or sides of ring (B); the fused pyrazole ring (C) is either in the 4,3- or the 3,4-arrangement; and tautomers of formula (I) compounds; when X is not oxygen, i.e. stands for sulphur or imino, Y may stand for a covalent bond that links the hydrogen directly to the carbon atom in position 2. Two methods for producing the novel formula (I) compounds are disclosed. The first or indazole method starts from a precursor having a benzene moiety (ring B) and a pyrazolo moiety (ring C) fused therewith, i.e. the indazole structure; ring (B) carries two vicinal substituents for forming the pyrimidine moiety or ring (A) by cyclization. The second or quinazoline method starts from a precursor having the pyrimidine moiety (A) and the benzene moiety (B) fused therewith, i.e. the quinazoline structure, and carrying two vicinal substituents for forming the pyrazole moiety (C) by cyclization. The first method, in addition to yielding the novel benzologs, provides for improved synthesis of previously disclosed benzo-allopurinols. Novel compounds of formula (I) are benzologs of such well known and biologically active compounds as oxipurinol, aminopurinol and thiopurinol and are expected to be applicable for comparable pharmaceutical purposes.

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First Claim