有机化学 ›› 2010, Vol. 30 ›› Issue (9): 1383-1386. 上一篇    下一篇

研究简报

6-氯哒嗪-3-甲酸甲酯的合成

陆秀宏,包雪飞,黄栗,戴文,魏巍,陈国良   

  1. (沈阳药科大学制药工程学院 沈阳 110016)
  • 收稿日期:2009-10-13 修回日期:2010-01-28 发布日期:2010-04-22
  • 通讯作者: 陈国良 E-mail:guoliang222@yahoo.com.cn

Synthesis of Methyl 6-Chloropyridazine-3-carboxylate

LU Xiu-Hong, BAO Xue-Fei, HUANG Li, DAI Wen, WEI Wei, CHEN Guo-Liang   

  1. (School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016)
  • Received:2009-10-13 Revised:2010-01-28 Published:2010-04-22

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.

关键词: 6-氯哒嗪-3-甲酸甲酯, 乙酰丙酸乙酯, 合成

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.

Key words: methyl 6-chloropyridazine-3-carboxylate, ethyl levulinate, synthesis