PURPOSE: To obtain a new adenosine kinase inhibitor made of a nucleoside analog having a specified molecular structure contg. a substd. purine skeleton, etc., having adenosine kinase inhibiting activity and useful as a treating for cardiovascular disease, cerebrovascular disease, etc., an anti-inflammatory drug, etc.
CONSTITUTION: 2',3'-(1-Methylethylidene)inosine is tosylated and allowed to react with sodium azide. The resultant 5'-azido-5'-deoxy-2',3'-O-(1- methylethylidene)inosine is chlorinated by reaction with SOCl2 in CH2Cl2 and the chlorinated product is allowed to react with amines, dissolved in HCO2H, diluted with water in a ratio of 1:1 and brought into reaction to obtain the objective compd. of the formula [where A is O, S or CH2; B' is (CH2)nB (1≤n≤4 and B is H, an alkyl, alkoxy, etc.); C1 and C2 are H, an acyl, etc.; X is C, etc.; Y is N or C; D is H, a halogen, alkyl, aryl, etc.; E is H, a halogen, alkyl, etc.; F is an alkyl, aryl, etc.; and G is H, a halogen, lower alkyl, etc.].
UGARKAR BHEEMARAO G (US)
MULLANE KEVIN M (US)
GRUBER HARRY E (US)
BULLOUGH DAVID A (US)
ERION MARK D (US)
CASTELLINO ANGELO (US)
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