Selective methylene C–H oxidation for the synthesis of alcohols with a broad scope and functional group tolerance is challenging due to the high proclivity for further oxidation of alcohols to ketones. Here, we report the selective synthesis of benzylic alcohols employing bis(methanesulfonyl) peroxide as an oxidant. We attempt to provide a rationale for the selectivity for monooxygenation, which is
[EN] POLYCYCLIC CAP-DEPENDENT ENDONUCLEASE INHIBITORS FOR TREATING OR PREVENTING INFLUENZA<br/>[FR] INHIBITEURS DE L'ENDONUCLÉASE DÉPENDANTE DE LA COIFFE POLYCYCLIQUES POUR LE TRAITEMENT OU LA PRÉVENTION DE LA GRIPPE
申请人:MERCK SHARP & DOHME
公开号:WO2022026285A1
公开(公告)日:2022-02-03
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing influenza. The compounds are cap-dependent endonuclease inhibitors.
Radical homopolymerization of linear α-olefins has been developed. The success of this polymerization relies on the high efficiency of 1,4-cyano group migration. This approach can be applied to homopolymerize α- substituted styrenes or acrylates. As a chain transfer agent, a symmetric allylic sulfide is created to regulate the propagating thiyl radicals over the polymerization process.
Nickel/Bis(oxazoline)-Catalyzed Asymmetric Negishi Arylations of Racemic Secondary Benzylic Electrophiles to Generate Enantioenriched 1,1-Diarylalkanes
作者:Hien-Quang Do、E. R. R. Chandrashekar、Gregory C. Fu
DOI:10.1021/ja408561b
日期:2013.11.6
A tertiary stereogenic center that bears two different aryl substituents is found in a variety of bioactive compounds, including medicines such as Zoloft and Detrol. We have developed an efficient method for the synthesis of enantioenriched 1,1-diarylalkanes from readily available racemic benzylic alcohols. Formation of a benzylic mesylate (which is not isolated), followed by treatment with an arylzinc reagent, LiI, and a chiral nickel/bis(oxazoline) catalyst, furnishes the Negishi cross-coupling product in high ee and good yield. A wide array of functional groups (e.g., an aryl iodide, a thiophene, and an N-Boc-indole) are compatible with the mild reaction conditions. This method has been applied to a gram-scale synthesis of a precursor to Zoloft.
Giampietro, Natalie C.; Wolfe, John P., Journal of the American Chemical Society, 2008, vol. 130, p. 12907 - 12911