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Ring-Closing Metathesis in Pharmaceutical Development: Fundamentals, Applications, and Future Directions
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2018-06-22 00:00:00 , DOI: 10.1021/acs.oprd.8b00093
Miao Yu 1 , Sha Lou 1 , Francisco Gonzalez-Bobes 1
Affiliation  

Ring-closing metathesis (RCM) has become indispensable in organic synthesis for both academic investigations and industrial applications. This review provides an overview of RCM reactions, focusing on the practical aspects that researchers in an industrial environment may find of interest. Key elements of reaction design and lessons learned from these applications are discussed to help those considering implementing RCM reactions on scale, particularly in manufacturing active pharmaceutical ingredients (APIs). Advances in the development of more effective catalysts and new methodologies, such as enantioselective RCM and stereoselective macrocyclic RCM, are also briefly discussed.

中文翻译:

药物开发中的闭环复分解:基本原理,应用和未来方向

对于学术研究和工业应用而言,闭环复分解(RCM)已成为有机合成中必不可少的。这篇综述概述了RCM反应,着重于工业环境中研究人员可能感兴趣的实践方面。讨论了反应设计的关键要素以及从这些应用中学到的教训,以帮助那些考虑大规模实施RCM反应的人员,特别是在制造活性药物成分(API)中。还简要讨论了开发更有效的催化剂和新方法的进展,例如对映选择性RCM和立体选择性大环RCM。
更新日期:2018-06-22
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