Diethanolamine Boronic Esters: Development of a Simple and Standard Process for Boronic Ester Synthesis,Organic Process Research & Development

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Diethanolamine Boronic Esters: Development of a Simple and Standard Process for Boronic Ester Synthesis
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-08-04 , DOI: 10.1021/acs.oprd.0c00296
Phillip A. Inglesby ₁ , Lauren R. Agnew ₁ , Holly L. Carter ₁ , Oliver T. Ring ₁

Affiliation

Herein, we disclose the unique physical properties of diethanolamine (DEA) boronic esters that have facilitated the development of a simple and standard process for their synthesis and isolation using environmentally sustainable solvents. Moreover, their preparation is facile, robust, and scalable and can be telescoped from a solution of boronic acid or boronic ester via esterification/transesterification with DEA, therefore providing wide access from a plethora of reaction types. To date, AstraZeneca has successfully manufactured three DEA boronic esters at the kilogram scale (5, 50, and 100 kg batches), with plans to expand this to more examples in 2020.

中文翻译：

二乙醇胺硼酸酯：硼酸酯合成的简单和标准方法的发展

本文中，我们公开了二乙醇胺（DEA）硼酸酯的独特物理性能，这些物理特性促进了使用环境可持续性溶剂合成和分离其简单标准工艺的发展。此外，它们的制备简便，稳定，可扩展，可以通过硼酸或硼酸酯溶液经DEA的酯化/酯交换反应进行伸缩，因此可以从多种反应类型中获得广泛的应用。迄今为止，阿斯利康已经成功生产了三种千克级DEA硼酸酯（5、50和100千克批次），并计划在2020年将其扩展到更多实例。

更新日期：2020-09-20

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