A highly convergent and efficient synthesis of a macrocyclic hepatitis C virus protease inhibitor BI 201302
A highly convergent large scale synthesis of a 15-membered macrocyclic hepatitis C virus (HCV) protease inhibitor BI 201302 was achieved, in which the key features are the practical macrocyclization by Ru-catalyzed ring-closing metathesis (0.1 mol % Grela catalyst, 0.1-0.2 M concentration) and the efficient sulfone-mediated SNAr reaction.
Wei, Xudong,Shu, Chutian,Haddad, Nizar,Zeng, Xingzhong,Patel, Nitinchandra D.,Tan, Zhulin,Liu, Jianxiu,Lee, Heewon,Shen, Sherry,Campbell, Scot,Varsolona, Richard J.,Busacca, Carl A.,Hossain, Azad,Yee, Nathan K.,Senanayake, Chris H.
supporting information
p. 1016 - 1019
(2013/04/10)
PROCESS FOR PREPARING SULFONYL QUINOLINES
Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are useful as intermediates in the preparation of potent active agents for the treatment of hepatitis C virus (HCV) infection.
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Page/Page column 16-17
(2010/10/03)
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