Design and Synthesis of Thromboxane Antagonists

• Main Authors: Ja-Ding Jan, 詹家鼎
• Other Authors: 陳清玉
• Format: Others
• Language: zh-TW
• Published: 1999
• Online Access: http://ndltd.ncl.edu.tw/handle/06556561254749991477

碩士 === 朝陽大學 === 應用化學研究所 === 87 === Thromboxane A2 is involved in many physiological functions. It is also the cause of many pathologicalconditions. For example: The increase in thromboxane A2 causes vascular contraction to produce atherosclerosis, thrombosis and asthma. The abnormal secretion of thromboxane A2 and platelet receptor activation may be one of the cause of thrombosis and atherosclerosis. Thromboxane antagonist may be a good approach to these diseases. According to past experience, potent thromboxane antagonist may contain the following pharmacophores, that is, a sulfonamide, an interphenylene ring and a carboxylic acid. The relative position of these three groups decided the potency of these antagonists. Synthesis of all these thromboxane antagonists, starting from Exo-7-Oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboxylic anhydride 12, were achieved in a short and convenient manner, leading to enantiopure compounds in good overall yields.