6-氯哒嗪-3-甲酸甲酯的合成

Synthesis of Methyl 6-Chloropyridazine-3-carboxylate

以乙酰丙酸乙酯为起始原料,经过环合、溴代、消除、重铬酸钾氧化、酯化、POCl3氯代6步反应合成6-氯哒嗪-3-甲酸甲酯,目标化合物总收率42%,本方法操作简单,成本低廉,分离纯化容易,收率高,为6-氯哒嗪-3-甲酸甲酯的规模化合成奠定了基础.

Methyl 6-chloropyridazine-3-carboxylate （1） is a key intermediate in the research of anti-tumor,blood-lipid lowering and insecticides. In this article,methyl 6-chloropyridazine-3-carboxylate （1） is synthesized by using ethyl levulinate as starting material via a six-steps process including cyclization,bromination,elimination,oxidation,esterification and chlorination in the overall yield of 42%. This method is easy to operate and purificate with good yield,and the starting material is cheap. It has established a way to prepare methyl 6-chloropyridazine-3-carboxylate （1） on a large scale.