抗癌新药L-651582的合成

Synthesis of L-651582

3,5-二氯苯甲酸经还原、TBDMSCl硅醚保护、酰化、脱保护和氯化制得3,5-二氯-4-(4-氯苯甲酰基)氯苄,再经叠氮化、与氰乙酰胺环合制得抗癌新药L-651582,总收率32%。

L-651582, an antiproliferative agent was synthesized from 3,5-dichlorobenzoic acid by reduction,protection, acylation, deprotection and chlorination to give 3,5-dichloro-4- （4-chlorobenzoyl） benzylchloride, which subjected to azidation and cyclization with cyanoacetamide in 32% overall yield.