Liquid‐Assisted Grinding Mechanochemistry in the Synthesis of Pharmaceuticals,Advanced Synthesis & Catalysis

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Liquid‐Assisted Grinding Mechanochemistry in the Synthesis of Pharmaceuticals
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2021-01-20 , DOI: 10.1002/adsc.202001245
Ping Ying ₁ , Jingbo Yu ₁ , Weike Su ₁

Affiliation

Mechanochemical reactions by milling, grinding or other types of mechanical action have emerged as a salient green approach because of its wide applications towards academic and industrial chemical communities in sustainable solvent‐free/solvent‐less processes. Liquid‐assisted grinding (LAG) as an extension of traditional solvent‐free mechanochemical techniques by which a small amount of liquid is used as an additive to enhance and/or control reactivity, has been fruitfully applied in the screening of inclusion compounds, cocrystals, salts, solvates, and polymorphs. However, utilization of this important technique in the synthesis of pharmaceutically and biologically relevant targets was not adequately investigated. This review article summarizes an overview of the latest development of LAG mechanochemical approaches in the synthesis of active pharmaceutical ingredients (API) and drug‐like fragments, highlights its superiority versus conventional syntheses.

中文翻译：

药物合成中的液体辅助研磨机械化学

通过研磨，研磨或其他类型的机械作用进行的机械化学反应已成为一种显着的绿色方法，因为它在可持续的无溶剂/无溶剂工艺中广泛应用于学术界和工业化学界。液体辅助研磨（LAG）是对传统无溶剂机械化学技术的扩展，通过使用少量液体作为添加剂来增强和/或控制反应性，已被成功地用于筛选夹杂物，共晶体，盐，溶剂化物和多晶型物。但是，没有充分研究这种重要技术在药物和生物学相关靶标的合成中的利用。

更新日期：2021-03-03

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