- In situ anionic shielding for regioselective metalation: Directed peri and iterative metalation routes to polyfunctionalized 7-azaindoles
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Strolling the ring: A general regioselective directed peri(C4)-metalation route to 1 through an in situ N-anionic protection of C2 is reported. The azaindoles may be elaborated by directed ortho metalation (DoM) and Suzuki coupling to more complex heterocyclic systems. An iterative ring-walk DoM sequence furnishes the exhaustively substituted 2. DMG=directed metalation group, TMEDA=N,N,N′,N′-tetramethylethylenediamine, TMS=trimethylsilyl. Copyright
- Schneider, Cedric,David, Emilie,Toutov, Anton A.,Snieckus, Victor
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supporting information; experimental part
p. 2722 - 2726
(2012/04/17)
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- Design and synthesis of human immunodeficiency virus entry inhibitors: Sulfonamide as an isostere for the α-ketoamide group
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The crystal structures of many tertiary α-ketoamides reveal an orthogonal arrangement of the two carbonyl groups. Based on the hypothesis that the α-ketoamide HIV attachment inhibitor BMS 806 (formally BMS378806, 26) might bind to its gp120 target via a s
- Lu, Rong-Jian,Tucker, John A.,Zinevitch, Tatiana,Kirichenko, Olga,Konoplev, Vitalii,Kuznetsova, Svetlana,Sviridov, Sergey,Pickens, Jason,Tandel, Sagun,Brahmachary, Enugurthi,Yang, Yang,Wang, Jian,Freel, Stephanie,Fisher, Shelly,Sullivan, Alana,Zhou, Jiying,Stanfield-Oakley, Sherry,Greenberg, Michael,Bolognesi, Dani,Bray, Brian,Koszalka, Barney,Jeffs, Peter,Khasanov, Alisher,Ma, You-An,Jeffries, Cynthia,Liu, Changhui,Proskurina, Tatiana,Zhu, Tong,Chucholowski, Alexander,Li, Rongshi,Sexton, Connie
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p. 6535 - 6544
(2008/09/16)
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