The Experts below are selected from a list of 10491 Experts worldwide ranked by ideXlab platform
Hongchao Guo - One of the best experts on this subject based on the ideXlab platform.
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asymmetric 3 3 annulation of copper allenylidenes with pyrazolones synthesis of chiral 1 4 dihydropyrano 2 3 c pyrazoles
Organic Letters, 2018Co-Authors: Feng Jiang, Xinping Feng, Rou Wang, Xing Gao, Hao Jia, Yumei Xiao, Cheng Zhang, Hongchao GuoAbstract:The copper-catalyzed asymmetric [3 + 3] annulation of Ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper–allenylidenes from Ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework.
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Asymmetric [3 + 3] Annulation of Copper–Allenylidenes with Pyrazolones: Synthesis of Chiral 1,4-Dihydropyrano[2,3‑c]pyrazoles
2018Co-Authors: Feng Jiang, Xinping Feng, Rou Wang, Xing Gao, Hao Jia, Yumei Xiao, Cheng Zhang, Hongchao GuoAbstract:The copper-catalyzed asymmetric [3 + 3] annulation of Ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper–allenylidenes from Ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework
Hiroaki Mitsuya - One of the best experts on this subject based on the ideXlab platform.
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delayed emergence of hiv 1 variants resistant to 4 Ethynyl 2 fluoro 2 deoxyadenosine comparative sequential passage study with lamivudine tenofovir emtricitabine and bms 986001
Antiviral Therapy, 2013Co-Authors: Kenji Maeda, Eiichi Kodama, Darshan V Desai, Manabu Aoki, Hirotomo Nakata, Hiroaki MitsuyaAbstract:Background4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) contains an Ethynyl moiety and the 3′-hydroxyl and exerts highly potent activity against various HIV type-1 (HIV-1) strains including multi-dr...
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a 4 c Ethynyl 2 3 dideoxynucleoside analogue highlights the role of the 3 oh in anti hiv active 4 c Ethynyl 2 deoxy nucleosides
Journal of Medicinal Chemistry, 2004Co-Authors: Maqbool A Siddiqui, Hiroaki Mitsuya, Stephen H Hughes, Paul L Boyer, Que N Van, Clifford George, Stefan G Sarafinanos, Victor E MarquezAbstract:4‘-C-Ethynyl-2‘-deoxynucleosides belong to a novel class of nucleoside analogues endowed with potent activity against a wide spectrum of HIV viruses, including a variety of resistant clones. Although favorable selectivity indices were reported for several of these analogues, some concern still exists regarding the 3‘-OH group and its role in cellular toxicity. To address this problem, we removed the 3‘-OH group from 4‘-C-Ethynyl-2‘-deoxycytidine (1a). This compound was chosen because of its combined high potency and low selectivity index. The removal of the 3‘-OH was not straightforward; it required a different synthetic approach from the one used to synthesize the parent compound. Starting with glycidyl-4-methoxyphenyl ether, the target 4‘-C-Ethynyl-2‘,3‘-dideoxycytidine analogue (rac-1h) was obtained after 13 steps. In a cellular assay, rac-1h was completely inactive (0.001−10 μM) against HIVLAI, demonstrating the critical importance of the 3‘-OH for antiviral activity. To determine whether the role of ...
Victor E Marquez - One of the best experts on this subject based on the ideXlab platform.
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a 4 c Ethynyl 2 3 dideoxynucleoside analogue highlights the role of the 3 oh in anti hiv active 4 c Ethynyl 2 deoxy nucleosides
Journal of Medicinal Chemistry, 2004Co-Authors: Maqbool A Siddiqui, Hiroaki Mitsuya, Stephen H Hughes, Paul L Boyer, Que N Van, Clifford George, Stefan G Sarafinanos, Victor E MarquezAbstract:4‘-C-Ethynyl-2‘-deoxynucleosides belong to a novel class of nucleoside analogues endowed with potent activity against a wide spectrum of HIV viruses, including a variety of resistant clones. Although favorable selectivity indices were reported for several of these analogues, some concern still exists regarding the 3‘-OH group and its role in cellular toxicity. To address this problem, we removed the 3‘-OH group from 4‘-C-Ethynyl-2‘-deoxycytidine (1a). This compound was chosen because of its combined high potency and low selectivity index. The removal of the 3‘-OH was not straightforward; it required a different synthetic approach from the one used to synthesize the parent compound. Starting with glycidyl-4-methoxyphenyl ether, the target 4‘-C-Ethynyl-2‘,3‘-dideoxycytidine analogue (rac-1h) was obtained after 13 steps. In a cellular assay, rac-1h was completely inactive (0.001−10 μM) against HIVLAI, demonstrating the critical importance of the 3‘-OH for antiviral activity. To determine whether the role of ...
Feng Jiang - One of the best experts on this subject based on the ideXlab platform.
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asymmetric 3 3 annulation of copper allenylidenes with pyrazolones synthesis of chiral 1 4 dihydropyrano 2 3 c pyrazoles
Organic Letters, 2018Co-Authors: Feng Jiang, Xinping Feng, Rou Wang, Xing Gao, Hao Jia, Yumei Xiao, Cheng Zhang, Hongchao GuoAbstract:The copper-catalyzed asymmetric [3 + 3] annulation of Ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper–allenylidenes from Ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework.
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Asymmetric [3 + 3] Annulation of Copper–Allenylidenes with Pyrazolones: Synthesis of Chiral 1,4-Dihydropyrano[2,3‑c]pyrazoles
2018Co-Authors: Feng Jiang, Xinping Feng, Rou Wang, Xing Gao, Hao Jia, Yumei Xiao, Cheng Zhang, Hongchao GuoAbstract:The copper-catalyzed asymmetric [3 + 3] annulation of Ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper–allenylidenes from Ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework
Maqbool A Siddiqui - One of the best experts on this subject based on the ideXlab platform.
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a 4 c Ethynyl 2 3 dideoxynucleoside analogue highlights the role of the 3 oh in anti hiv active 4 c Ethynyl 2 deoxy nucleosides
Journal of Medicinal Chemistry, 2004Co-Authors: Maqbool A Siddiqui, Hiroaki Mitsuya, Stephen H Hughes, Paul L Boyer, Que N Van, Clifford George, Stefan G Sarafinanos, Victor E MarquezAbstract:4‘-C-Ethynyl-2‘-deoxynucleosides belong to a novel class of nucleoside analogues endowed with potent activity against a wide spectrum of HIV viruses, including a variety of resistant clones. Although favorable selectivity indices were reported for several of these analogues, some concern still exists regarding the 3‘-OH group and its role in cellular toxicity. To address this problem, we removed the 3‘-OH group from 4‘-C-Ethynyl-2‘-deoxycytidine (1a). This compound was chosen because of its combined high potency and low selectivity index. The removal of the 3‘-OH was not straightforward; it required a different synthetic approach from the one used to synthesize the parent compound. Starting with glycidyl-4-methoxyphenyl ether, the target 4‘-C-Ethynyl-2‘,3‘-dideoxycytidine analogue (rac-1h) was obtained after 13 steps. In a cellular assay, rac-1h was completely inactive (0.001−10 μM) against HIVLAI, demonstrating the critical importance of the 3‘-OH for antiviral activity. To determine whether the role of ...
