Department of Chemistry & Pharmaceutical Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
Chem Commun (Camb). 2010 Nov 14;46(42):7918-20. doi: 10.1039/c0cc02823a. Epub 2010 Sep 20.
A very short and efficient synthesis of the important drug candidate telaprevir, featuring a biocatalytic desymmetrization and two multicomponent reactions as the key steps, is presented. The classical issue of lack of stereoselectivity in Ugi- and Passerini-type reactions is circumvented. The atom economic and convergent nature of the synthetic strategy require only very limited use of protective groups.
介绍了一种非常简短高效的重要药物候选物特拉匹韦的合成方法，其关键步骤包括生物催化的不对称拆分和两个多组分反应。该合成方法避免了 Ugi 和 Passerini 型反应中缺乏立体选择性的经典问题。合成策略的原子经济性和汇聚性只需要非常有限地使用保护基团。
