162109-00-4Relevant articles and documents
Development of a pilot-plant process for a nevirapine analogue HIV NNRT inhibitor
Busacca, Carl A.,Cerreta, Mike,Dong, Yong,Eriksson, Magnus C.,Farina, Vittorio,Feng, XuWu,Kim, Ji-Young,Lorenz, Jon C.,Sarvestani, Max,Simpson, Robert,Varsolona, Rieh,Vitous, Jana,Campbell, Scot J.,Davis, Mark S.,Jones, Paul-James,Norwood, Daniel,Qiu, Fenghe,Beaulieu, Pierre L.,Duceppe, Jean-Simon,Hache, Bruno,Brong, Jim,Chiu, Fang-Ting,Curtis, Tom,Kelley, Jason,Lo, Young S.,Powner, Tory H.
, p. 603 - 613 (2013/01/03)
The pilot-plant synthesis of nevirapine analogue 1 is described. The compound was prepared in eight steps from substituted pyridine raw materials and 4-hydroxyquinoline. The key transformation involves a novel one-pot conversion of an arylhalide to arylac
Non-nucleoside reverse transcriptase inhibitors
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Page 9, (2010/02/07)
Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
Non-nucleoside reverse transcriptase inhibitors
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, (2008/06/13)
Provided are compounds of the general formula I: wherein R2 is selected from the group consisting of H, F, Cl, (C1-4) alkyl, (C3-4) cycloalkyl and CF3; R4 is H or Me; R5 is H, Me or Et, wit
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones
Proudfoot,Patel,Kapadia,Hargrave
, p. 1406 - 1410 (2007/10/02)
We have explored the potential of derivatives of the dipyrido[2,3- b:2',3'-e][1,4]diazepinone ring system as inhibitors of HIV-1 reverse transcriptase (RT). These compounds are isomeric to the potent RT inhibitor nevirapine and are available via a novel Smiles rearrangement on intermediates used for the synthesis of nevirapine analogs. Derivatives of this isomeric series are weaker inhibitors of RT than corresponding nevirapine analogs, although with appropriate substitution of the A- and C- pyridine rings activity can be improved.