The Synthesis of 8-Substituted Purine Derivatives. I. Some 8-Substituted Derivatives of Hypoxanthine.

Abstract

Some hypoxanthine derivatives which were substituted at C₈-position by hydrophilic groups such as-SH, -S-CH₂-COOH, -COOH, -CH₂OH and-CH₂-CH₂-COOH were synthesized for testing purine-antagonist action. They were prepared by condensation of 4, 5-diamino-6-hydroxypyrimidine (I) with the corresponding acid or amide compounds through the acyl derivatives of (I). A direct preparation of 4-amino-6-hydroxypyrimidine by reaction of malonamamidine with ethyl formate was also described.