881674-85-7Relevant academic research and scientific papers
Development and Scope of the Arene-Fused Domino Michael/Mannich Reaction: Application to the Total Syntheses of Aspidosperma Alkaloids (-)-Aspidospermidine, (-)-Tabersonine, and (-)-Vincadifformine
Zhao, Senzhi,Andrade, Rodrigo B.
, p. 521 - 531 (2017/04/26)
The development and application of the arene-fused domino Michael/Mannich route to the tetrahydrocarbazole (ABE) core of Aspidosperma alkaloids is described. The scope of this novel transformation was studied in terms of the nucleophilic component (i.e., N-sulfinyl metallodienamine) and the electrophilic component (i.e., Michael acceptor). The successful application of this methodology toward the concise total syntheses of classical indole alkaloids (-)-aspidospermidine, (-)-tabersonine, and (-)-vincadifformine in 10-11 steps, respectively, is also discussed.
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors
Johnson, Ted W.,Tanis, Steven P.,Butler, Scott L.,Dalvie, Deepak,Delisle, Dorothy M.,Dress, Klaus R.,Flahive, Erik J.,Hu, Qiyue,Kuehler, Jon E.,Kuki, Atsuo,Liu, Wen,McClellan, Guy A.,Peng, Qinghai,Plewe, Michael B.,Richardson, Paul F.,Smith, Graham L.,Solowiej, Jim,Tran, Khanh T.,Wang, Hai,Yu, Xiaoming,Zhang, Junhu,Zhu, Huichun
experimental part, p. 3393 - 3417 (2011/07/08)
Figure Presented. HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the synthesis of orally bioavailable azaindole hydroxamic acids that were potent inhibitors of the HIV-1 IN enzyme. Here we disclose the design and synthesis of novel tricyclic N-hydroxy-dihydronaphthyridinones as potent, orally bioavailable HIV-1 integrase inhibitors displaying excellent ligand and lipophilic efficiencies.
INHIBITORS OF THE HIV INTEGRASE ENZYME
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Page/Page column 55, (2010/11/27)
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.
