The olefin metathesis reaction is finding increasing use in drug discovery and process chemistry, with a number of applications now implemented at commercial manufacturing scale. Catalyst improvements over the past decade have allowed use of the metathesis reaction with highly functionalized substrates, allowing chemists to access increasingly diverse chemical space, including most notably macrocycles, constrained small ring spirocycles, and fused-ring systems. For scientists employed in the pharmaceutical industry, the patent literature is the primary avenue for communication of synthetic routes to drug candidates. While most examples of the metathesis reaction in the patent literature offer only sketchy experimental details and provide little context on reaction development, the wide scope of substrates within the pharmaceutical patent literature provides a true indication of reaction scope and functional group compatibility. The current article reviews applications of the metathesis reactions in drug discovery and development in the pharmaceutical industry disclosed in the patent literature from January 2016 to August 2017.

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药物发现和开发中的烯烃复分解—来自最近专利文献的例子

烯烃复分解反应正在药物发现和过程化学中得到越来越多的应用，目前已在商业规模上实现了许多应用。在过去十年中，催化剂的改进使易位反应可以与高度官能化的底物一起使用，从而使化学家能够进入日益多样化的化学空间，包括最著名的大环，受限的小环螺环和稠环系统。对于制药行业的科学家而言，专利文献是将合成路线传达给候选药物的主要途径。尽管专利文献中有关复分解反应的大多数示例仅提供了粗略的实验细节，并且几乎没有提供反应发展的背景信息，药物专利文献中底物的广泛范围提供了反应范围和官能团相容性的真实指示。本文回顾了复分解反应在2016年1月至2017年8月专利文献中公开的制药行业药物发现和开发中的应用。