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Recent advances in synthetic approaches for medicinal chemistry of C-nucleosides

机译:C-核苷药物化学合成方法的最新进展

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摘要

C-nucleosides have intrigued biologists and medicinal chemists since their discovery in 1950's. In that regard, C-nucleosides and their synthetic analogues have resulted in promising leads in drug design. Concurrently, advances in chemical syntheses have contributed to structural diversity and drug discovery efforts. Convergent and modular approaches to synthesis have garnered much attention in this regard. Among them nucleophilic substitution at C1' has seen wide applications providing flexibility in synthesis, good yields, the ability to maneuver stereochemistry as well as to incorporate structural modifications. In this review, we describe recent reports on the modular synthesis of C-nucleosides with a focus on D-ribonolactone and sugar modifications that have resulted in potent lead molecules.
机译:自1950年代发现以来,C-核苷一直引起生物学家和药用化学家的兴趣。在这方面,C-核苷及其合成类似物已在药物设计中带来了有希望的线索。同时,化学合成的进步促进了结构的多样性和药物发现的努力。在这方面,融合的和模块化的合成方法已经引起了很多关注。其中C1'处的亲核取代已获得广泛应用,从而提供了合成灵活性,高收率,操纵立体化学的能力以及结合结构修饰的能力。在这篇综述中,我们描述了有关C-核苷模块合成的最新报告,重点是D-核糖内酯和糖修饰,这些修饰已导致有效的先导分子。

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