Liu Wanyi
2008
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Journal
Chinese Journal of Pharmaceuticals
Abstract
2-Amino-6-cyclopropylamino-9H-purine,the key intermediate of abacavir was synthesized from ethyl cyanoacetate by nitrosation,cyclization with guanidine hydrochloride in the presence of EtONa and reduction to give 2,4,5-triamino-6-hydroxypyrimidine,which was subjected to cyclization with formic acid,acylation,chlorination and condensation with cyclopropylamine with an overall yield of about 39%.