Chem. J. Chinese Universities ›› 1981, Vol. 2 ›› Issue (2): 183.

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SYNTHESIS OF N-ETHYLPERHEXILINE MALEATE AND PERHEXILINE MALEATE

Li Liangzhu   

  1. Department of Chemistry, Beijing University, Beijing
  • Received:1980-01-21 Online:1981-04-24 Published:1981-04-24

Abstract: Anew 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.

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