【摘要】 沛心达是近年来很受重视的一个新型的防治冠心病的有效药物。我们在研究新的合成方法,由1,1-苯基-2-(2-吡啶基)乙烯进行催化氢化制备沛心达时,发现伴有N-乙基沛心达生成。经质谱、红外光谱和元素分析等试验证明了它的结构为1,1-二环己基-2-(2-N-乙基哌啶基)乙烷马来酸盐。由沛心达游离碱进行N-乙基化,也取得了相同的结果。并由药理试验表明,N-乙基沛心达有希望成为一个更好的心血管药物。更多还原

【Abstract】 A new compound N-ethylperhexiline maleate (Ⅱ) is isolated duringthe synthesis of perhexiline maleate (I), which has been known as an effective drug in the treatment of coronary atherosclerosis. Studies of its m. s., IR. and element analysis prove that it has the structure as indicated by (Ⅱ). (Ⅱ) was also prepared by alkylation of the free base of perhexiline maleate. Its pharmocologic test is shown to be more effective than ( I ) when it is used as an anti-arrhythmic agent.The new route of synthesis is by condensing of benzophenone with 2-methylpyridine in the presence of sodamide giving 1,1-diphenyl-2- (2-pyri-dyl) ethanol (Ⅲ), which is dehydrated to yield 1 ,1-diphenyl-2-(2-pyridyl) ethene (Ⅳ), followed by complete hydrogenation in ethanol and then treated with maleic acid to form perhexiline maleate ( I ) and N-ethylperhexiline maleate (Ⅱ). The yields of (I) and (II) are 43% and 11% repectively.更多还原