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Synthon Approach in Designing Organic Synthesis: A Case Study of Rational Synthesis Design of a Potent Antidiabetic Agent 'RosigIitazone.'

机译:有机合成设计中的Synthon方法:以有效的抗糖尿病药“ RosigIitazone”为例,合理合成设计为例。

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摘要

Synthon approach advocated by Prof. E. J. Corey of Harvard University has emerged as a powerful analytical tool of design synthetic routes for the preparation of an organic compound of any interest from readily available starting materials. This approach plays a vital role in the synthesis of medicinal compounds/drugs which is a part and parcel of modern drug discovery process. Taking the privilege of this approach, a good number of synthesis schemes has been proposed for a potent anti-diabetic agent "rosiglitazone" keeping an overview on the works published in both journals and patent literatures. The proposed synthesis planning being a theoretical investigation, the actual laboratory execution requires the cross examination of a considerable number of factors such as reactions, reagents and order of events. In actual practice, generally that route is most feasible which is cost-effective, safe, and easy to carry out and produces maximum yield in a short reaction time.
机译:哈佛大学E. J. Corey教授倡导的Synthon方法已成为设计合成路线的强大分析工具,可以从容易获得的起始原料制备任何感兴趣的有机化合物。这种方法在合成药用化合物/药物中起着至关重要的作用,这是现代药物发现过程的重要组成部分。利用这种方法的优势,已经提出了许多有效的抗糖尿病药物“罗格列酮”的大量合成方案,并对其在期刊和专利文献中发表的工作进行了概述。拟议的综合计划是一项理论研究,实际的实验室执行需要对相当多的因素(例如反应,试剂和事件顺序)进行交叉检查。在实际实践中,通常该路线是最可行的,其成本有效,安全且易于实施,并在较短的反应时间内产生最大的收率。

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