球磨机
酰胺
胺气处理
化学
组合化学
活性成分
溶剂
有机化学
机械化学
化学工程
生物信息学
工程类
生物
作者
William I. Nicholson,Fabien Barreteau,Jamie A. Leitch,Riley Payne,Ian Priestley,Edouard Godineau,Claudio Battilocchio,Duncan L. Browne
标识
DOI:10.1002/ange.202106412
摘要
Abstract The direct mechanochemical amidation of esters by ball milling is described. The operationally simple procedure requires an ester, an amine, and substoichiometric KOtBu and was used to prepare a large and diverse library of 78 amide structures with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochemical protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochemicals as well as the gram‐scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent.
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