In Pursuit of Synthetic Efficiency: Convergent Approaches,Accounts of Chemical Research

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In Pursuit of Synthetic Efficiency: Convergent Approaches
Accounts of Chemical Research ( IF 16.4 ) Pub Date : 2021-01-15 , DOI: 10.1021/acs.accounts.0c00727
Yang Gao ₁ , Dawei Ma ₁

Affiliation

The field of total synthesis has reached a stage in which emphasis has been increasingly focused on synthetic efficiency rather than merely achieving the synthesis of a target molecule. The pursuit of synthetic efficiency, typically represented by step count and overall yield, is a rich source of inspiration and motivation for synthetic chemists to invent innovative strategies and methods. Among them, convergent strategy has been well recognized as an effective approach to improve efficiency. This strategy generally involves coupling of fragments with similar complexity to furnish the target molecule via subsequent cyclization or late-stage functionalization. Thus, methodologies that enable effective connection of fragments are critical to devising a convergent plan. In our laboratory, convergent strategy has served as a long-standing principle for pursuing efficient synthesis during the course of planning and implementing synthetic projects. In this Account, we summarize our endeavors in the convergent synthesis of natural products over the last ten years. We show how we identify reasonable bond disconnections and employ enabling synthetic methodologies to maximize convergency, leading to the efficient syntheses of over two-dozen highly complex molecules from eight disparate families.

中文翻译：

追求综合效率：趋同方法

全合成领域已经达到了一个阶段，在该阶段中，越来越多的重点放在合成效率上，而不是仅仅实现目标分子的合成。对合成效率的追求（通常以步数和总产量表示）是合成化学家发明创新策略和方法的丰富灵感和动力来源。其中，融合策略已被公认为提高效率的有效方法。该策略通常涉及偶联具有相似复杂性的片段，以通过随后的环化或后期功能化来提供靶分子。因此，实现片段有效连接的方法对于设计收敛计划至关重要。在我们的实验室在规划和实施综合项目的过程中，融合策略一直是追求高效综合的长期原则。在此报告中，我们总结了过去十年中天然产物聚合合成的努力。我们展示了如何确定合理的键断开连接并采用可行的合成方法来最大程度地收敛，从而有效地合成了来自八个不同家族的两对以上高度复杂的分子。

更新日期：2021-02-02

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