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绿色促进技术在药物先导化合物竞争合成中的应用。

Green Enabling Technologies for Competitive Synthesis of Pharmaceutical Lead Compounds.

机构信息

Dipartimento di Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, Italy.

First Moscow State Medical University (Sechenov), Inst. Translational Medicine and Biotechnology, 8 Trubetskaya ul, Moscow, Russian Federation.

出版信息

Curr Pharm Des. 2020;26(44):5700-5712. doi: 10.2174/1381612826999201116163951.

Abstract

Combinations of different technologies are at the heart of the development and implementation of new, innovative processes and approaches for Industry 4.0 in the field of medicinal chemistry and drug discovery. Process intensification and advances in high-throughput synthetic techniques can dramatically improve reaction rates in processes for which slow kinetics represents a bottleneck. Easier access to target-based chemical library collections offers wider access to new leads for drug development. Green enabling technologies are a reliable ally for the design of environmentally friendly synthetic processes and more highly competitive pharmaceutical production. Mechanochemistry, microwaves, ultrasound and flow chemistry are mature techniques that can boast drug synthesis when properly integrated into the production chain. In this review, we selected examples from the literature of the last five years related to medicinal chemistry.

摘要

不同技术的组合是药物化学和药物发现领域中工业 4.0 新的创新流程和方法的开发和实施的核心。工艺强化和高通量合成技术的进步可以极大地提高反应速率,这些反应的动力学较慢是一个瓶颈。基于靶标的化学文库收集更容易获得新的药物开发先导化合物。绿色使能技术是设计环保合成工艺和更具竞争力的制药生产的可靠盟友。机械化学、微波、超声和流动化学是成熟的技术,当它们被恰当地整合到生产链中时,可以用于药物合成。在这篇综述中,我们从过去五年的文献中选择了与药物化学相关的例子。

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