Second-Generation Process for the HCV Protease Inhibitor BILN 2061: A Greener Approach to Ru-Catalyzed Ring-Closing Metathesis†

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• 作者：Vittorio Farina*^&#167 ; ; Chutian Shu* ; Xingzhong Zeng ; Xudong Wei ; Zhengxu Han ; Nathan K. Yee ; Chris H. Senanayake*
• 刊名：Organic Process Research & Development
• 出版年：2009
• 出版时间：March 20, 2009
• 年：2009
• 卷：13
• 期：2
• 页码：250-254
• 全文大小：160K
• 年卷期：v.13,no.2(March 20, 2009)
• ISSN：1520-586X

文摘

The ring-closing metathesis (RCM) step, a key reaction in our process to BILN 2061, was dramatically improved from the first-generation process by the selection of a more appropriate substrate as well as the use of a more effective catalyst. The two RCM reactions are compared in detail using criteria that are of high significance to the process chemist.