Zarganes-Tzitzikas Tryfon, Dömling Alexander
Org Chem Front. 2014 Sep 1;1(7):834-837. doi: 10.1039/C4QO00088A.
Multicomponent reaction (MCR) technology is now widely recognized for its impact on drug discovery projects and is strongly endorsed by industry as well as academia. However, still relatively few products based on MCRs are marketed or under development. This provides tremendous opportunities for organic chemists to shorten synthetic pathways thus reducing the cost-of-goods considerably. A recent example of the HCV drug Telaprevir is highlighted where introduction of two MCRs could lead to a shortening of the synthesis route by more than 50%.
多组分反应(MCR)技术因其对药物发现项目的影响而得到广泛认可,并受到业界和学术界的大力支持。然而,基于MCR的产品仍相对较少进入市场或处于研发阶段。这为有机化学家提供了巨大的机会,可缩短合成途径,从而大幅降低商品成本。文中重点介绍了丙肝药物特拉匹韦的一个最新例子,引入两个MCR可使合成路线缩短50%以上。