血管紧张素Ⅱ受体拮抗剂坎地沙坦酯的合成研究

【作者】 景士云；

【导师】 宫平；

【作者基本信息】 沈阳药科大学 ， 药物化学， 2003， 硕士

【摘要】 本论文是关于血管紧张素Ⅱ受体AT₁拮抗剂——坎地沙坦西来昔替酯的合成研究。 本论文简述了高血压的危害及抗高血压药物的发展概况，详细介绍了血管紧张素Ⅱ受体AT₁拮抗剂的进展及AT₁拮抗剂坎地沙坦酯的作用机制，着重研究了坎地沙坦酯的合成。设计并打通了坎地沙坦酯的合成路线，并对其合成工艺进行了较为详尽的考察和改进，缩短了反应步骤，并使操作简便、收率提高。合成路线以3-硝基-1，2-苯二甲酸为起始原料，经酯化、氯化、Curtius重排、烃化、还原、两步环合、水解、酯化、转晶共十步反应后，得到了C-晶型坎地沙坦酯，总收率（以3-硝基-1，2-苯二甲酸计）为6.8％。 坎地沙坦酯的结构经红外光谱、紫外光谱、核磁共振氢谱、核磁共振碳谱、质谱得以确证，进行了差热分析，并经红外光谱、X-射线衍射分析确定其晶型。更多还原

【Abstract】 The synthetic process of a new angiotensin II receptor antagonist, Candesartan cilexetil was studied in this paper.The danger of hypertension and the development of antihypertensive agents were briefly described in this paper. Both the development of angiotensin II receptor antagonists and the characteristics of Candesartan cilexetil were introduced. The synthesis of Candesartan cilexetil was studied particularly. The synthetic route was designed and modified, which made easier to process. The action steps were shortened and the yield was elevated. The total yield of Candesartan cilexetil was 6.8%, which was synthesized from 3-nitrophthalic acid by ten steps. The structure of Candesartan cilexetil was confirmed by IR, UV, ¹H-NMR, ¹³C-NMR, MS, DSC, and its C-crystal form was confirmed by IR and X-ray.更多还原