Enantioselective Transformations in the Synthesis of Therapeutic Agents.
Enantioselective Transformations in the Synthesis of Therapeutic Agents.
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DOI：
10.1021/acs.chemrev.3c00010
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发表时间：
2023-07
期刊：
影响因子：
62.1
通讯作者：
He Yang;Hanxiao Yu;I. Stolarzewicz;Wenjun Tang
中科院分区：
文献类型：
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作者：
He Yang;Hanxiao Yu;I. Stolarzewicz;Wenjun Tang
在过去的二十年里，已批准的手性药物和医学研究中的候选药物的比例急剧上升。因此，对映体纯药物或其合成中间体的有效合成对药物和过程化学家提出了巨大的挑战。不对称催化的重大进展为这一挑战提供了有效且可靠的解决方案。过渡金属催化、有机催化和生物催化在医药工业中的成功应用，通过高效、精准地制备对映体富集的治疗剂，促进了药物发现，并促进了活性药物成分以经济、环保的方式工业化生产。本综述总结了不对称催化在制药行业的最新应用（2008-2022），范围从工艺规模到中试和工业水平。它还展示了利用最先进的不对称催化技术不对称合成治疗药物的最新成果和趋势。
The proportion of approved chiral drugs and drug candidates under medical studies has surged dramatically over the past two decades. As a consequence, the efficient synthesis of enantiopure pharmaceuticals or their synthetic intermediates poses a profound challenge to medicinal and process chemists. The significant advancement in asymmetric catalysis has provided an effective and reliable solution to this challenge. The successful application of transition metal catalysis, organocatalysis, and biocatalysis to the medicinal and pharmaceutical industries has promoted drug discovery by efficient and precise preparation of enantio-enriched therapeutic agents, and facilitated the industrial production of active pharmaceutical ingredient in an economic and environmentally friendly fashion. The present review summarizes the most recent applications (2008-2022) of asymmetric catalysis in the pharmaceutical industry ranging from process scales to pilot and industrial levels. It also showcases the latest achievements and trends in the asymmetric synthesis of therapeutic agents with state of the art technologies of asymmetric catalysis.