402958-24-1Relevant articles and documents
Telaprevir intermediate preparation method
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, (2017/08/31)
The invention discloses a telaprevir intermediate preparation method. A telaprevir intermediate is a formula I compound, and a reaction route is as shown in the specification, wherein R is selected from C1-C4 alkyl groups, R1 is selected from hydrogen, C1-C8 alkyl groups, C1-C8 alkoxy groups, C6-C12 aryl groups, alkyl sulfonyl, C6-C12 aryl sulfonyl groups or substituted C6-C12 aryl sulfonyl groups, and P is an amino protection group. The method has advantages of simplicity in operation, safety, freeness of pollution and special requirements on equipment, low production cost, high yield and the like, is suitable for large-scale production and has a high practical value in realization of telaprevir industrialization.
Discovery of a novel bicycloproline P2 bearing peptidyl α-ketoamide LY514962 as HCV protease inhibitor
Yip, Yvonne,Victor, Frantz,Lamar, Jason,Johnson, Robert,Wang, Q. May,Barket, Donna,Glass, John,Jin, Ling,Liu, Lifei,Venable, Daryl,Wakulchik, Mark,Xie, Congping,Heinz, Beverly,Villarreal, Elcira,Colacino, Joe,Yumibe, Nathan,Tebbe, Mark,Munroe, John,Chen, Shu-Hui
, p. 251 - 256 (2007/10/03)
We describe herein the design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles.