The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Shun-yi Wang - One of the best experts on this subject based on the ideXlab platform.
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Mn(III)-Mediated Cascade Cyclization of 3-Isocyano-[1,1'-biphenyl]-2-carbonitrile with Arylboronic Acid: Construction of Pyrrolopyridine Derivatives.
Organic letters, 2019Co-Authors: Yi-ming Zhu, Fei Wang, Shun-yi WangAbstract:A Mn(III) mediated cascade cyclization of new designed multifunctionalized 3-isocyano-[1,1′-biphenyl]-2-carbonitrile with arylboronic acid to construct Pyrrolopyridine derivatives is developed. A series of pyrroloporidine compounds have been constructed through the formation of two new C–C bonds and one C–N bond via a radical pathway.
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Mn(III)-Mediated Cascade Cyclization of 3‑Isocyano-[1,1′-biphenyl]-2-carbonitrile with Arylboronic Acid: Construction of Pyrrolopyridine Derivatives
2019Co-Authors: Yi-ming Zhu, Fei Wang, Shun-yi WangAbstract:A Mn(III) mediated cascade cyclization of new designed multifunctionalized 3-isocyano-[1,1′-biphenyl]-2-carbonitrile with arylboronic acid to construct Pyrrolopyridine derivatives is developed. A series of pyrroloporidine compounds have been constructed through the formation of two new C–C bonds and one C–N bond via a radical pathway
Yi-ming Zhu - One of the best experts on this subject based on the ideXlab platform.
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Mn(III)-Mediated Cascade Cyclization of 3-Isocyano-[1,1'-biphenyl]-2-carbonitrile with Arylboronic Acid: Construction of Pyrrolopyridine Derivatives.
Organic letters, 2019Co-Authors: Yi-ming Zhu, Fei Wang, Shun-yi WangAbstract:A Mn(III) mediated cascade cyclization of new designed multifunctionalized 3-isocyano-[1,1′-biphenyl]-2-carbonitrile with arylboronic acid to construct Pyrrolopyridine derivatives is developed. A series of pyrroloporidine compounds have been constructed through the formation of two new C–C bonds and one C–N bond via a radical pathway.
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Mn(III)-Mediated Cascade Cyclization of 3‑Isocyano-[1,1′-biphenyl]-2-carbonitrile with Arylboronic Acid: Construction of Pyrrolopyridine Derivatives
2019Co-Authors: Yi-ming Zhu, Fei Wang, Shun-yi WangAbstract:A Mn(III) mediated cascade cyclization of new designed multifunctionalized 3-isocyano-[1,1′-biphenyl]-2-carbonitrile with arylboronic acid to construct Pyrrolopyridine derivatives is developed. A series of pyrroloporidine compounds have been constructed through the formation of two new C–C bonds and one C–N bond via a radical pathway
Richard J. Fox - One of the best experts on this subject based on the ideXlab platform.
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c h arylation in the formation of a complex Pyrrolopyridine the commercial synthesis of the potent jak2 inhibitor bms 911543
Journal of Organic Chemistry, 2019Co-Authors: Richard J. Fox, Lopa Bakrania, Carolyn S. Wei, Neil A. Strotman, Michael B. Hay, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Nicolas Cuniere, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials.
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C–H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543
The Journal of organic chemistry, 2018Co-Authors: Richard J. Fox, Cuniere Nicolas, Lopa Bakrania, Carolyn S. Wei, Neil A. Strotman, Michael B. Hay, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials.
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C–H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543
2018Co-Authors: Richard J. Fox, Lopa Bakrania, Neil A. Strotman, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Nicolas Cuniere, Carolyn Wei, Michael Hay, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials
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Ni-Catalyzed C–H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
The Journal of organic chemistry, 2015Co-Authors: Monica A Fitzgerald, Carolyn S. Wei, Omid Soltani, Dimitri Skliar, Bin Zheng, Jacob Albrecht, Michael A. Schmidt, Michelle Mahoney, Richard J. FoxAbstract:BMS-911543 is a complex Pyrrolopyridine investigated as a potential treatment for myeloproliferative disorders. The development of a short and efficient synthesis of this molecule is described. During the course of our studies, a Ni-mediated C–N bond formation was invented, which enabled the rapid construction of the highly substituted 2-aminopyridine core. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only eight steps starting from readily available materials.
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Ni-Catalyzed C–H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
2015Co-Authors: Monica A Fitzgerald, Carolyn Wei, Omid Soltani, Dimitri Skliar, Bin Zheng, Jacob Albrecht, Michelle Mahoney, Michael Schmidt, Richard J. FoxAbstract:BMS-911543 is a complex Pyrrolopyridine investigated as a potential treatment for myeloproliferative disorders. The development of a short and efficient synthesis of this molecule is described. During the course of our studies, a Ni-mediated C–N bond formation was invented, which enabled the rapid construction of the highly substituted 2-aminopyridine core. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only eight steps starting from readily available materials
Terrence R. Burke - One of the best experts on this subject based on the ideXlab platform.
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Bicyclic hydroxy-1H-Pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
Chemical biology & drug design, 2011Co-Authors: Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Métifiot, Steven J. Smith, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. BurkeAbstract:HIV-1 integrase (IN) is a validated therapeutic target for the treatment of AIDS. However, the emergence of resistance to raltegravir, the sole marketed FDA-approved IN inhibitor, emphasizes the need to develop second-generation inhibitors that retain efficacy against clinically relevant IN mutants. We report herein bicyclic hydroxy-1H-Pyrrolopyridine-triones as a new family of HIV-1 integrase inhibitors that were efficiently prepared using a key ‘Pummerer cyclization deprotonation cycloaddition’ cascade of imidosulfoxides. In in vitro HIV-1 integrase assays, the analogs showed low micromolar inhibitory potencies with selectivity for strand transfer reactions as compared with 3′-processing inhibition. A representative inhibitor (5e) retained most of its inhibitory potency against the three major raltegravir-resistant IN mutant enzymes, G140S/Q148H, Y143R, and N155H. In antiviral assays employing viral vectors coding these IN mutants, compound 5e was approximately 200- and 20-fold less affected than raltegravir against the G140S/Q148H and Y143R mutations, respectively. Against the N155H mutation, 5e was approximately 10-fold less affected than raltegravir. Thus, our new compounds represent a novel structural class that may be further developed to overcome resistance to raltegravir, particularly in the case of the G140S/Q148H mutations.
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Development of tricyclic hydroxy-1H-Pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters, 2011Co-Authors: Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Métifiot, Steven J. Smith, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. BurkeAbstract:New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3′-processing.
Michael Lawler - One of the best experts on this subject based on the ideXlab platform.
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c h arylation in the formation of a complex Pyrrolopyridine the commercial synthesis of the potent jak2 inhibitor bms 911543
Journal of Organic Chemistry, 2019Co-Authors: Richard J. Fox, Lopa Bakrania, Carolyn S. Wei, Neil A. Strotman, Michael B. Hay, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Nicolas Cuniere, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials.
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C–H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543
The Journal of organic chemistry, 2018Co-Authors: Richard J. Fox, Cuniere Nicolas, Lopa Bakrania, Carolyn S. Wei, Neil A. Strotman, Michael B. Hay, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials.
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C–H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543
2018Co-Authors: Richard J. Fox, Lopa Bakrania, Neil A. Strotman, Dayne Fanfair, Christopher S. Regens, Gregory L. Beutner, Nicolas Cuniere, Carolyn Wei, Michael Hay, Michael LawlerAbstract:The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex Pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials
