1155270-69-1Relevant articles and documents
Concise and Practical Asymmetric Synthesis of a Challenging Atropisomeric HIV Integrase Inhibitor
Fandrick, Keith R.,Li, Wenjie,Zhang, Yongda,Tang, Wenjun,Gao, Joe,Rodriguez, Sonia,Patel, Nitinchandra D.,Reeves, Diana C.,Wu, Jiang-Ping,Sanyal, Sanjit,Gonnella, Nina,Qu, Bo,Haddad, Nizar,Lorenz, Jon C.,Sidhu, Kanwar,Wang, June,Ma, Shengli,Grinberg, Nelu,Lee, Heewon,Tsantrizos, Youla,Poupart, Marc-André,Busacca, Carl A.,Yee, Nathan K.,Lu, Bruce Z.,Senanayake, Chris H.
, p. 7144 - 7148 (2015/06/16)
Abstract A practical and efficient synthesis of a complex chiral atropisomeric HIV integrase inhibitor has been accomplished. The combination of a copper-catalyzed acylation along with the implementation of the BI-DIME ligands for a ligand-controlled Suzuki cross-coupling and an unprecedented bis(trifluoromethane)sulfonamide-catalyzed tert-butylation renders the synthesis of this complex molecule robust, safe, and economical. Furthermore, the overall synthesis was conducted in an asymmetric and diastereoselective fashion with respect to the imbedded atropisomer. Atropselective: An efficient asymmetric synthesis of an atropisomeric HIV inhibitor has been accomplished. The combination of a copper-catalyzed acylation with the implementation of BI-DIME ligands for a ligand-controlled Suzuki cross-coupling and an unprecedented bis(trifluoromethane)sulfonamide-catalyzed tert-butylation renders the synthesis of this complex molecule robust, safe, and economical.
THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS
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, (2010/12/17)
The present invention relates to a series of compounds of formula (A) having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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, (2009/06/27)
Compounds of formula I : wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.