舒尼替尼的合成工艺研究

Synthesis of Sunitinib

以乙酰乙酸乙酯为原料,经Knorr反应、选择性水解、脱羧、甲酰化、水解及缩合得标题化合物。6步总收率为31.1%,各步中间体及目标物结构经MS和1HNMR确证。改进后的方法缩短了步骤、简化了操作、降低了成本,适合于放大制备。

To synthesize Sunitinib as antitumor agent.Target compound was synthesized by using ethyl acetoacetate as starting material via Knorr reaction,selective hydrolysis,decarboxylation,formylation,hydrolysis and condensation.The total yield of the six steps was 31.1% and the structures of the intermediates and the target compound were confirmed by MS and 1HNMR analysis.This improved method is of many advantages,such as simple steps,easy operation,low cost,which can be feasible to large-scale preparation.