第 37 卷第 6 期Vol. 37 No. 6
2007 年 12 月Dec 2007

所属栏目:农药及中间体

2-氯烟酸的合成
陈建辉,吴志刚,沈大冬,胡建香 (浙江医药股份有限公司 新昌制药厂,浙江 新昌 312500)
摘 要:综述了2-氯烟酸的合成工艺,并提出了改进的工艺路线。3-氰基吡啶先经乙酰丙酮酸钼催化氧化得到烟酸N-氧化物,再经有机碱和苯磷酰二氯作用下,三氯氧磷氯化得到2-氯烟酸,总收率95.0%。
关键词:2-氯烟酸;合成;乙酰丙酮酸钼;苯磷酰二氯
中图分类号:O626.32  文献标识码:A  文章编号:1009-9212(2007)06- 0019-03
ynthesis of 2-Chloronicotinic Acid
CHEN Jian-hui,WU Zhi-gang,SHEN Da-dong,HU Jian-xiang (Xinchang Pharmaceutical Factory, Zhejiang Medicine Co., Ltd.,Xinchang 312500, China)
Abstract:An improved synthetic process of 2-chloronicotinic acid was reported based on reviewing its synthetic processes in detail. 3-cyanopyridine was oxidized to nicotinic acid N-oxide using molybdenyl acetylacetonate as catalyst, and then chloridized to give the title product 2-chloronicotinic acid through chlorination by POCl3 in presence of organic base and phenyl dichlorophosphate(PDCP). The total yield of 2-chloronicotinic acid was 95%.
Key words:2-chloronicotinic acid; synthesis; molybdenyl acetylacetonate; phenyldichlorophosphate
作者简介:陈建辉(1971-),男,浙江新昌人,高级工程师,从事新药合成。(E-mail:chenjianhui-2005@sohu.com)
收稿日期:2007-10-16