4-甲基烟腈衍生物的合成研究  

Synthesis of 5-substituted Derivatives of 4-methylnicotinonitrile

作　　者：刘津[1] 冯启国[1] 张杨[1] 赵毅民[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《解放军药学学报》2011年第4期283-285,共3页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：十一五国家新药创制重大专项;No.2009ZX09301-002

摘　　要：目的合成4-甲基烟腈衍生物。方法以4-甲基-5-乙烯基烟腈为原料,经臭氧化/还原、氯代、wittig反应和酸水解等步骤合成新的5位取代目标化合物。结果合成了4个未见文献报道的4-甲基烟腈衍生物,收率均在70%以上,产物的化学结构经MS和1H-NMR确证。结论所用合成方法简便易行、条件温和,产物可用于合成含吡啶环的生物碱。Objective To synthesize 4-methylnicotinonitrile derivatives.Methods New 5-substituted derivatives of 4-methylnicotinonitrile were synthesized through ozonization-reduction,chloration,wittig-reaction and acidic hydrolyzation using 4-methyl-5-vinylnicotinonitrile as the starting material.Results Four new compounds were synthesized with a yield of over 70%.Their structures were verified by MS and 1H-NMR.Conclusion This synthetic procedure is user-friendly under mild reaction conditions and the product can be used in the synthesis of pyridine-type alkaloids.

关 键 词：4-甲基-5-羟甲基烟腈 4-甲基-5-氯甲基烟腈 4-甲基-5-醛基烟腈 4-甲基-5-乙醛基烟腈 合成 

分 类 号：R914.5[医药卫生—药物化学]