A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions

作者：Znabet Anass; Polak Marloes M; Janssen Elwin; de Kanter Frans J J; Turner Nicholas J; Orru Romano V A; Ruijter Eelco^*

来源：Chemical Communications, 2010, 46(42): 7918-7920.

DOI：10.1039/c0cc02823a

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.

• 出版日期2010