| 抗帕金森病药Istradefylline的合成 |
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| 引用本文： | 李凡,侯兴普,李林,律涛,杜玉民. 抗帕金森病药Istradefylline的合成[J]. 中国医药工业杂志, 2010, 41(4) |
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| 作者姓名： | 李凡 侯兴普 李林 律涛 杜玉民 |
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| 作者单位： | 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 |
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| 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).
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| 关 键 词： | 抗帕金森病药 腺苷A_(2a)受体拮抗剂 合成 |
Synthesis of Antiparkinsonian Agent Istradefylline |
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| Abstract: | Istradefylline, the antiparkinsonian agent, was synthesized from vanillin via methylation, Knoevenagel condensation and chlorination by SOCl_2 to give (E) -3,4-dimethoxy cinnamoyl chloride, which was subjected to amidation with l,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). |
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| Keywords: | istradefylline istradefylline antiparkinsonian agent adenosine A_(2a) receptor inhibitor synthesis |
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