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继1975年硝苯啶在德国上市后,又上市了5个新的二氢吡啶类药物,即非洛地平、伊拉地平、尼卡地平、尼莫地平和尼群地平。尼伐地平也已于去年注册。对二氢吡啶类的研究,目的在于寻找新的强效及长效降压药,本品是这类药物中最有希望的。合成邻苯二醛(Ⅰ)与Ⅱ在二氯甲烷中进行Wittig缩合,得3-(2-甲酰基苯基)-2(E)-丙烯酸特丁酯(Ⅲ),然后Ⅲ在醋酸中与3-氨基丁烯酸乙酯(Ⅳ)环合即得。药理作用本品是一个新的血管选择性钙拮抗剂,具有高效和长效的降压活性。家兔K~+去极化耳动脉标本体外试验
Following the listing of nifedipine in Germany in 1975, five new dihydropyridines, namely felodipine, isradipine, nicardipine, nimodipine and nitrendipine, were listed. Nilvatipine was registered last year. Dihydropyridines research, the purpose is to find new potent and long-acting antihypertensive drugs, this product is the most promising of these drugs. Wittig condensation of o-phthalaldehyde (I) and II in dichloromethane yields 3- (2-formylphenyl) -2 (E) -tertbutyl acrylate (III) 3 - aminocrotonic acid ethyl ester (IV) ring that is too. Pharmacological effects This product is a new vascular selective calcium antagonist, with high efficiency and long-lasting antihypertensive activity. Rabbit K ~ + depolarized ear artery in vitro test