抗帕金森病药Istradefylline的合成  

Synthesis of Antiparkinsonian Agent Istradefylline

作　　者：李凡[1] 侯兴普 李林[1] 律涛[1] 杜玉民[1] 

机构地区：[1]河北医科大学药学院,河北石家庄050017 [2]石药集团恩必普药业有限公司,河北石家庄052160

出　　处：《中国医药工业杂志》2010年第4期241-243,共3页Chinese Journal of Pharmaceuticals

摘　　要：香草醛经甲基化、Knoevenagel缩合、氯化亚砜氯代得(E)-3,4-二甲氧基苯丙烯酰氯,再与1,3-二乙基-5,6-二氨基尿嘧啶(7)经酰胺化、闭环及甲基化反应制得抗帕金森病药istradefylline。7可由N,N'-二乙基脲和氰乙酸经缩合闭环、亚硝化及还原反应制得。总收率约54%(以N,N'-二乙基脲计)。Istradefylline, the antiparkinsonian agent, was synthesized from vanillin via methylation, Knoevenagel condensation and chlorination by SOCl2 to give （E）-3,4-dimethoxy cinnamoyl chloride, which was subjected to amidation with 1,3-diethyl-5,6-diaminouracil（7）, followed by cyclization and methylation. Compound 7 was prepared from N,N ＇-diethylurea and cyanoacetic acid by condensation, cyclization, nitrosation and reduction. The overall yield was about 54%（based on N,N＇-diethylurea）.

关 键 词：istradefylline 抗帕金森病药 腺苷A2a受体拮抗剂 合成 

分 类 号：R971.5[医药卫生—药品]