RCM Macrocyclization Made Practical:  An Efficient Synthesis of HCV Protease Inhibitor BILN 2061

We report here that dramatic improvement of the key RCM reaction in the synthesis of HCV protease inhibitor BILN2061 can be achieved by N-substitution of the diene substrate with an electron-withdrawing group. Mechanistic studies using 1H NMR spectroscopy showed an unprecedented switch of the initia...

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Veröffentlicht in:	Organic letters 2008-03, Vol.10 (6), p.1303-1306
Hauptverfasser:	Shu, Chutian, Zeng, Xingzhong, Hao, Ming-Hong, Wei, Xudong, Yee, Nathan K, Busacca, Carl A, Han, Zhengxu, Farina, Vittorio, Senanayake, Chris H
Format:	Artikel
Sprache:	eng
Schlagworte:	Carbamates - chemistry Cyclization Hepacivirus - enzymology Macrocyclic Compounds - chemistry Protease Inhibitors - chemistry Quinolines - chemistry Thiazoles - chemistry
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