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Total synthesis of bryostatins: The development of methodology for the atom-economic and stereoselective synthesis of the ring C subunit

机译:bryostatins的全合成:环C亚基的原子经济和立体选择性合成方法的发展

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Bryostatins, a family of structurally complicated macrolides, exhibit an exceptional range of biological activities. The limited availability and structural complexity of these molecules makes development of an efficient total synthesis particularly important. This article describes our initial efforts towards the total synthesis of bryostatins, in which chemoselective and atom-economical methods for the stereoselective assembly of the ring C subunit were developed. A Pd-catalyzed tandem alkyne-alkyne coupling/6-endo-dig cyclization sequence was explored and successfully pursued in the synthesis of a dihydropyran ring system. Elaboration of this methodology ultimately led to a concise synthesis of the ring C subunit of bryostatins.
机译:抑霉菌素是结构复杂的大环内酯类药物,具有广泛的生物活性。这些分子的有限的可用性和结构复杂性使得开发有效的全合成尤为重要。本文介绍了我们对全抑素抑制素的初步研究,其中开发了化学选择性和原子经济的方法用于环C亚基的立体选择性组装。在二氢吡喃环系统的合成中,探索并成功地探索了Pd催化的串联炔烃-炔烃偶联/ 6-内-dig环化序列。对该方法的详细说明最终导致了bryostatins环C亚基的简洁合成。

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