Search Results - "Bolduc, Philippe N."
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Synthesis of N‑Substituted 3‑Amino-2-pyridones
Published in Organic letters (26-08-2022)“…Pyridones are versatile building blocks in organic synthesis and a privileged motif in drug discovery. However, N-substituted 2-pyridones bearing an α-tertiary…”
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2
Overcoming Limitations in Decarboxylative Arylation via Ag–Ni Electrocatalysis
Published in Journal of the American Chemical Society (28-09-2022)“…A useful protocol for achieving decarboxylative cross-coupling (DCC) of redox-active esters (RAE, isolated or generated in situ) and halo(hetero)arenes is…”
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Carbon quaternization of redox active esters and olefins by decarboxylative coupling
Published in Science (American Association for the Advancement of Science) (05-04-2024)“…The synthesis of quaternary carbons often requires numerous steps and complex conditions or harsh reagents that act on heavily engineered substrates. This is…”
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The Discovery of 7‑Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)‑N‑(6-methylpyrazolo[1,5‑a]pyrimidin-3-yl)imidazo[1,2‑a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke
Published in Journal of medicinal chemistry (28-03-2024)“…Interleukin receptor-associated kinase 4 (IRAK4) is a key node of signaling within the innate immune system that regulates the production of inflammatory…”
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Discovery of BIO-8169A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation
Published in Journal of medicinal chemistry (23-05-2024)“…Interleukin receptor associated kinase 4 (IRAK4) plays an important role in innate immune signaling through Toll-like and interleukin-1 receptors and…”
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Synthesis of Unnatural Amino Acids via Ni/Ag Electrocatalytic Cross-Coupling
Published in Organic letters (22-03-2024)“…A simple protocol is outlined herein for rapid access to enantiopure unnatural amino acids (UAAs) from trivial glutamate and aspartate precursors. The method…”
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Complex molecule synthesis by electrocatalytic decarboxylative cross-coupling
Published in Nature (London) (23-11-2023)“…Modern retrosynthetic analysis in organic chemistry is based on the principle of polar relationships between functional groups to guide the design of synthetic…”
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Nickel‐Electrocatalytic Decarboxylative Arylation to Access Quaternary Centers
Published in Angewandte Chemie International Edition (19-02-2024)“…There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling of tertiary alkyl fragments to…”
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A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors
Published in ACS medicinal chemistry letters (09-05-2024)“…We herein report the discovery, synthesis, and evolution of a series of indazoles and azaindazoles as CNS-penetrant IRAK4 inhibitors. Described is the use of…”
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10
Nickel‐Electrocatalytic Decarboxylative Arylation to Access Quaternary Centers
Published in Angewandte Chemie (19-02-2024)“…There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling of tertiary alkyl fragments to…”
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