抗 SARS-CoV-2 药物 Ensitrelvir 合成策略综述

IF 3.1 3区 化学 Q2 CHEMISTRY, APPLIED Organic Process Research & Development Pub Date : 2024-05-01 DOI:10.1021/acs.oprd.3c00494
Yuanchang Liu, Gaorong Wu, Yiting Yang, Wei Hu, Xiaopeng Peng, Zihan Peng, Jiatao Xia, Xin Xie, Jiuzhong Huang* and Weiming Chen*, 
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摘要

严重急性呼吸系统综合征冠状病毒 2(SARS-CoV-2)的爆发和迅速传播导致了 21 世纪以来最严重的公共卫生危机之一。通过不同策略合成的口服抗 SARS-CoV-2 药物 ensitrelvir 具有令人满意的抗病毒效果。本综述从程序、产量、杂质、安全性和环境等方面总结了目前报道的恩西瑞韦以及三种相关关键构件衍生物合成策略的优缺点。这将为进一步的工艺开发和药物发现提供一个新的视角。
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Comprehensive Review on the Synthetic Strategies toward Anti-SARS-CoV-2 Drug Ensitrelvir

The outbreak and rapid spread of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) have led to one of the most serious public health crises since the beginning of the 21st century. An oral anti-SARS-CoV-2 drug ensitrelvir was developed with satisfactory antiviral effect and was synthesized via different strategies. This Review summarizes the advantages and disadvantages of the currently reported synthetic strategies for ensitrelvir along with three related key building blocks derivatives from the view of procedure, yield, impurities, safety, and environment. This will provide a novel perspective for further process development and drug discovery.

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来源期刊
CiteScore
6.90
自引率
14.70%
发文量
251
审稿时长
2 months
期刊介绍: The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools,process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.
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