- Borohydride reduction stabilizing system and method for reducing ester into alcohol
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The invention provides a borohydride reduction stabilizing system and a method for reducing ester into alcohol. The borohydride reduction stabilizing system comprises a borohydride reducing agent anda stabilizer for stabilizing the borohydride reducing agent, wherein the borohydride reducing agent is sodium borohydride or potassium borohydride, and the stabilizer is an alkali metal salt of alcohol. On the basis of an existing sodium borohydride/potassium reducing agent, an alcohol alkali metal salt (such as sodium alcoholate or potassium alcoholate) is added, and then the sodium borohydride/potassium reducing agent can keep stable and is not decomposed under a heating condition, so that on one hand, reduction activity is maintained in a relatively high state and the situation of excessiveuse is reduced, and on the other hand, generation of hydrogen is reduced and the process risk is reduced.
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Paragraph 0128; 0129; 0130
(2019/09/13)
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- Synthesis and biological evaluation of phosphonate analogues of nevirapine
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A series of nevirapine-based analogues containing the phosphonate functionality were prepared and evaluated in vitro against HIV RT. The effect of the phosphonate was evaluated against the wild type and Y181C HIV replication. An in vivo PK study was perfo
- Parrish, Jay,Tong, Leah,Wang, Michael,Chen, Xiaowu,Lansdon, Eric B.,Cannizzaro, Carina,Zheng, Xubin,Desai, Manoj C.,Xu, Lianhong
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p. 1493 - 1497
(2013/03/14)
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- Development of a pilot-plant process for a nevirapine analogue HIV NNRT inhibitor
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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
- 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.
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p. 603 - 613
(2013/01/03)
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- Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors
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A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus. Our efforts have resulted in a series of benzoic acid analogues that are potent inhibitors of HIV-1 replication against a panel of HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs). Furthermore, the combination of good antiviral potency, a broad spectrum of activity, and an excellent pharmacokinetic profile provides strong justification for the further development of compound 7 as a potential treatment for wild type and NNRT1-resistant HIV-1 infection.
- O'Meara, Jeff A.,Yoakim, Christiane,Bonneau, Pierre R.,B?s, Michael,Cordingley, Michael G.,Déziel, Robert,Doyon, Louise,Duan, Jianmin,Garneau, Michel,Guse, Ingrid,Landry, Serge,Malenfant, Eric,Naud, Julie,Ogilvie, William W.,Thavonekham, Bounkham,Simoneau, Bruno
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p. 5580 - 5588
(2007/10/03)
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- Non-nucleoside reverse transcriptase inhibitors
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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.
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- Non-nucleoside reverse transcriptase inhibitors
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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
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