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使用连续流动化学合成活性药物成分(原料药)。

The synthesis of active pharmaceutical ingredients (APIs) using continuous flow chemistry.

作者信息

Baumann Marcus, Baxendale Ian R

机构信息

Department of Chemistry, Durham University, South Road, DH1 3LE Durham, United Kingdom.

出版信息

Beilstein J Org Chem. 2015 Jul 17;11:1194-219. doi: 10.3762/bjoc.11.134. eCollection 2015.

DOI:10.3762/bjoc.11.134
PMID:26425178
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4578405/
Abstract

The implementation of continuous flow processing as a key enabling technology has transformed the way we conduct chemistry and has expanded our synthetic capabilities. As a result many new preparative routes have been designed towards commercially relevant drug compounds achieving more efficient and reproducible manufacture. This review article aims to illustrate the holistic systems approach and diverse applications of flow chemistry to the preparation of pharmaceutically active molecules, demonstrating the value of this strategy towards every aspect ranging from synthesis, in-line analysis and purification to final formulation and tableting. Although this review will primarily concentrate on large scale continuous processing, additional selected syntheses using micro or meso-scaled flow reactors will be exemplified for key transformations and process control. It is hoped that the reader will gain an appreciation of the innovative technology and transformational nature that flow chemistry can leverage to an overall process.

摘要

连续流动处理作为一项关键使能技术的应用,改变了我们进行化学研究的方式,并扩展了我们的合成能力。因此,人们设计了许多新的制备路线来合成具有商业价值的药物化合物,实现了更高效、可重复的生产。这篇综述文章旨在阐述流动化学在制备药物活性分子方面的整体系统方法和多样应用,展示该策略在从合成、在线分析与纯化到最终制剂与压片等各个方面的价值。尽管本综述将主要聚焦于大规模连续处理,但对于关键转化和过程控制,也将举例说明使用微尺度或中尺度流动反应器的其他选定合成方法。希望读者能领略到流动化学可应用于整个过程的创新技术及其变革性本质。

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