【摘 要】
：
苯并硫氮杂卓是一类具有镇静作用的合成药物，对精神病，心脏病及高血压等疾病有一定疗效。为了深入探讨其结构与药效关系，应用１Ｈ１ＨＣＯＳＹ，１３Ｃ１ＨＣＯＳＹ和ＮＯＥＳＹ等２ＤＮＭＲ技术对苯并硫氮杂卓１及其环加成产物２～５进行了研
【机 构】
：
北京医科大学药学院,兰州大学化学系
【出 处】
：
Journal of Chinese Pharmaceutical Sciences
论文部分内容阅读
苯并硫氮杂卓是一类具有镇静作用的合成药物，对精神病，心脏病及高血压等疾病有一定疗效。为了深入探讨其结构与药效关系，应用１Ｈ１ＨＣＯＳＹ，１３Ｃ１ＨＣＯＳＹ和ＮＯＥＳＹ等２ＤＮＭＲ技术对苯并硫氮杂卓１及其环加成产物２～５进行了研究，对其１Ｈ、１３ＣＮＭＲ化学位移进行了指定，并分析讨论了化合物１～５的结构特征及苯并硫氮七元杂环呈船式构象的特点，各相关质子间的偶合常数也与讨论结果相符
Benzothiazepine is a class of sedative synthetic drugs that have some effect on diseases such as psychosis, heart disease and high blood pressure. In order to further explore the relationship between its structure and pharmacodynamics, benzothiazepine 1 and its cycloaddition products 2-5 were studied by 2D NMR techniques such as 1H1HCOSY, 13C1HCOSY and NOESY. The 1H, 13CNMR chemistry The structures of compounds 1 ~ 5 and the characteristics of ship-like conformations of 7-membered heterocycle of benzothiazepine were analyzed and discussed. The coupling constants of all the related protons were also consistent with the results of the discussion
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