Effective Utilization of Flow Chemistry: Use of Unstable Intermediates, Inhibition of Side Reactions, and Scale-Up for Boronic Acid Synthesis,Organic Process Research & Development

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Effective Utilization of Flow Chemistry: Use of Unstable Intermediates, Inhibition of Side Reactions, and Scale-Up for Boronic Acid Synthesis
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-05-30 00:00:00 , DOI: 10.1021/acs.oprd.8b00118
Hirotsugu Usutani _{1,

2} , David G. Cork ₁

Affiliation

Flow chemistry processes for boronic acid syntheses utilizing lithiation–borylation have been developed. The side reactions in the lithiation step that occur in batch were suppressed, and unstable lithium intermediates were handled safely. Flow technology was applied to several kinds of boronic acid syntheses, and scale-up was successfully conducted to allow kilogram-scale production. Some of the key benefits of flow flash chemistry were utilized, both to avoid side reactions and to enable dianion chemistry that is difficult to perform successfully in batch reactions. The examples showed further perspectives on the utility of flow technologies for process development.

中文翻译：

流动化学的有效利用：不稳定的中间体的使用，副反应的抑制以及硼酸合成的放大

已经开发出利用锂化-硼化的硼酸合成流程化学方法。锂化步骤中分批发生的副反应得到抑制，并且安全处理了不稳定的锂中间体。流技术已应用于多种硼酸合成中，并成功进行了规模放大以实现千克规模的生产。利用了流动闪蒸化学的一些关键优点，既避免了副反应，又使难于在批量反应中成功进行的二价阴离子化学成为可能。这些示例进一步展示了流程技术在流程开发中的实用性。

更新日期：2018-05-30

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