Cross-couplings are among the most frequently used reactions in complex molecule synthesis. However, the requirement of stoichiometric base can cause challenges. Harsh, insoluble inorganic bases can lead to poor tolerance of sensitive functional groups, scale-up issues, and difficult adaptation to continuous flow platforms. Herein, we describe the use of high throughput experimentation to identify a number of conditions that enable Buchwald–Hartwig reactions to be carried out using readily available ligands (e.g., XantPhos) with DBU as a soluble, functional-group-tolerant, homogeneous base. Application of this system to diverse aminations in batch and flow are demonstrated, as is the translation of this technique to performing continuous Mizoroki–Heck and Sonogashira coupling reactions.

中文翻译：

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探索批次和流动中轻度布赫瓦尔德-哈特维希胺胺化的均相条件

交叉偶联是复杂分子合成中最常用的反应之一。但是，化学计量基准的要求可能会带来挑战。苛刻的不溶性无机碱可能导致敏感官能团的耐受性差，规模扩大问题，以及难以适应连续流动平台。本文中，我们描述了使用高通量实验来确定许多条件，这些条件使Buchwald-Hartwig反应能够使用易于获得的配体（例如XantPhos）与DBU作为可溶的，耐官能团的，均质的碱进行。演示了该系统在批量和流动性胺化反应中的应用，以及该技术在进行连续的Mizoroki-Heck和Sonogashira偶联反应中的转化。