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Dopropidil是一种抗心绞痛的钙拮抗剂。合成在氮气下向热的2-甲基-1-丙醇(Ⅱ)加入三氟化硼乙醚化物溶液,再加入1-氯-2,3-环氧丙烷(Ⅰ)。加入吡咯烷(Ⅳ)得Ⅴ,Ⅴ以亚硫酰氯氯化得Ⅵ,1-丙快基-1-环己醇(Ⅶ)与Ⅵ缩合(在甲苯和氢氧化钠水溶液中)即得Dopropidil[EP 031171,US4430332]。药理作用本品是一种结构新颖的抗心绞痛的钙拮抗剂。在离体兔主动脉环标本上本品拮抗K~+引起的收缩的浓度是1.3±0.2μM,与苄普地尔(bepridil)等效。对离体大
Dopropidil is a calcium antagonist against angina pectoris. Synthesis To a hot solution of 2-methyl-1-propanol (II) under nitrogen was added a solution of boron trifluoride etherate followed by 1-chloro-2,3-epoxypropane (I). Pyrrolidine (IV) is added to obtain V, V is chlorinated with thionyl chloride to give VI, and 1-propan-1-ylcyclohexanol (VII) is condensed with VI in toluene and aqueous sodium hydroxide to obtain Dopropidil [ EP 031171, US4430332]. Pharmacological effects This product is a novel structure of anti-angina calcium antagonist. In isolated rabbit aortic ring specimens of the product antagonistic K ~ + -induced contraction concentration of 1.3 ± 0.2μM, and bepridil (bepridil) equivalent. On the big body