恩他卡朋的合成  

Synthesis of entacapone

作　　者：熊远珍[1] 吴淑芳[2] 周南进[2] 

机构地区：[1]复旦大学药学院,上海200032 [2]江西医学院药学系,江西南昌330006

出　　处：《中国现代应用药学》2005年第6期456-456,共1页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的用改进的方法合成及纯化恩他卡朋,提高产率。方法以3,4-二羟基-5-硝基苯甲醛和N,N-二乙基-氰基酰胺为原料,在弱碱性条件下经过克脑文格尔反应生成2-氰基-N,N-二乙基-3-(3,4-二羟基-5-硝基苯基)丙烯酰胺,然后对顺反异构体进行纯化,最后进行红外光谱分析,元素分析,X-射线粉末衍射分析。结果所合成的终产物图谱与标品一致。OBJECTIVE In order to increase product rate, new way has been taken to prepare and purify entacapone. METHOD 3,4-dihydroxy-5-nitro-benzaldehyde was used to react with N, N-diethylcyanoacetamide, between which taking place knoevengal reaction in base condition, the crude product 2-cyano-N, N-diethyl-3-（ 3,4dihydroxy-5-nitrophenl） acrylamide was purified to obtain E-isomer, the result product was analyzed, such as element analysis, X-ray power diffraction analysis and infrared spectrum. RESULT The spectrum of result product is the same as standard compound.

关 键 词：恩他卡朋 合成 几何异构 纯化 

分 类 号：TQ460.6[化学工程—制药化工]