A method for synthesis of the important intermediates of Olmesartan

来源 :2015年全国药物化学学术会议暨第五届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:bigwbiso
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  Objective To synthesize the important intermediates of Olmesartan.Methods 2-propyl-1H-imidazole-4,5-dicarboxylic acid diethyl ester was synthesized using tartaric acid,an easily available,inexpensive and renewable substrate,as starting material via nitration,cyclization,esterifcation Results The technics was improved and toxic material was replaced.
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核苷类似物是一类重要的抗肿瘤和抗病毒药物。核苷类抗肿瘤药物的研究表明,通过改变分子糖基侧链可以使药物的抗肿瘤活性有很大的提高,同时还可以降低药物的毒副作用。由于氟原子的体积小且具有强烈的电负性,能参与氢键作用,因此在核苷的糖基上连接氟原子会影响整个核苷结构的电子分布,使其化学稳定性增加。