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近年来发现的肾上腺素能β-受体阻断剂如1-(3,4-二氯代苯基)-2-异丙氨基乙醇(DCI,I),丙萘醇(pronethalol,nethalide,II)能对抗心律不齐,治疗心绞痛等心血管系统疾病.I的毒性过高,不适于临床应用,II的作用专一性不如I,且有致癌性.我们设想II的作用专一性不够,可能由于其萘环结构与去甲肾上腺素的儿茶酚母核差别较大.我们合成了6-(2-异丙氨基-1-羟基乙基)-1,4-苯并二氧己环(III),并设想苯并-1,二氧杂己环与儿茶酚比较接近,更可视为儿茶酚的环醚衍生物,但又保持着II的二个六元并环特征.许多已知抗肾上腺素药物如吡并生(piperoxan)等也有苯并-1,4-二氧杂己环结构.
Adrenergic beta-blockers found in recent years such as 1- (3,4-dichlorophenyl) -2-isopropylaminoethanol (DCI, I), propethalol (nethalide, II ) Can fight against arrhythmia, angina pectoris and other cardiovascular diseases.I toxicity is too high, not suitable for clinical application, the specificity of II is not as good as I, and carcinogenic.We assume that the specificity of II is not enough, May be due to its naphthalene ring structure and norepinephrine catecholamine core difference we have synthesized 6- (2-isopropylamino-1-hydroxyethyl) -1,4-benzodioxan (III). It is assumed that benzo-1, dioxetane and catechol are closer and more likely to be regarded as cyclic ether derivatives of catechol, while retaining the two six-membered ring characteristics of II. Many known anti-adrenergic drugs such as piperoxan and the like also have a benzo-1,4-dioxane ring structure.