Greening the Valsartan Synthesis: Scale-up of Key Suzuki鈥揗iyaura Coupling over SiliaCat DPP-Pd

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• 作者：Valerica Pandarus ; Delphine Desplantier-Giscard ; Genevi猫ve Gingras ; Fran莽ois B茅land ; Rosaria Ciriminna ; Mario Pagliaro
• 刊名：Organic Process Research & Development
• 出版年：2013
• 出版时间：December 20, 2013
• 年：2013
• 卷：17
• 期：12
• 页码：1492-1497
• 全文大小：232K
• 年卷期：v.17,no.12(December 20, 2013)
• ISSN：1520-586X

文摘

The study of the scale-up of the heterogeneous Suzuki-Miyaura coupling reaction in batch conditions between 2-chlorobenzonitrile and 4-tolylboronic acid, a key step in valsartan synthesis, to produce 4鈥?methyl-2-biphenylcarbonitrile over the SiliaCat DPP-Pd catalyst in ethanol under reflux allows to identify the optimal reaction conditions. The catalyst, regardless of limited Pd leaching, is not reusable, and the method can be effectively applied to the high yield synthesis of several coupling products, opening the route to efficient continuous coupling syntheses.