Studies on Chemotherapeutic Agents.III. A Synthesis of 3-Phenylpurine Derivatives

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1-Phenyl-5, 6-diaminouracil (IX) or-2-thiouracil (X) prepared from 1-phenyl-6-aminouracil (V) or 1-phenyl-6-amino-2-thiouracil (VI) in an usual way was fused with urea or thiourea to yield 3-phenyluric acid and 3-phenylthiouric acid derivatives (XII, XIII, XIV and XV), while it was reacted with formamide to afford 3-phenylxanthine derivatives (XX and XXI), and with nitrous acid to give triazolo-derivatives (XXIV and XXV). Acetylation of IX or X resulted in formation of the corresponding 5-acetyl derivatives (XXVII and XXVIII) which on heating at 230∼240° as the sodium salts were converted into 8-methylpurine derivatives (XXIX and XXX). Preliminary anti-cancer testing results of the purine derivatives synthesized were described.

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