Search Results - "Witten, Michael R."
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Catalytic Asymmetric Synthesis of 8-Oxabicyclooctanes by Intermolecular [5+2] Pyrylium Cycloadditions
Published in Angewandte Chemie International Edition (02-06-2014)“…Highly enantioselective intermolecular [5+2] cycloadditions of pyrylium ion intermediates with electron‐rich alkenes are promoted by a dual catalyst system…”
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Journal Article -
2
Dual Catalysis in Enantioselective Oxidopyrylium-Based [5 + 2] Cycloadditions
Published in Journal of the American Chemical Society (21-09-2011)“…A new method for effecting catalytic enantioselective intramolecular [5 + 2] cycloadditions based on oxidopyrylium intermediates is reported. The dual catalyst…”
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Journal Article -
3
Rhodium(III)-Catalyzed Imidoyl C–H Activation for Annulations to Azolopyrimidines
Published in Organic letters (20-04-2018)“…Azolopyrimidines are efficiently prepared by direct imidoyl C–H bond activation. Annulations of N-azolo imines with sulfoxonium ylides and diazoketones under…”
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Journal Article -
4
A Simple Primary Amine Catalyst for Enantioselective α‑Hydroxylations and α‑Fluorinations of Branched Aldehydes
Published in Organic letters (05-06-2015)“…A new primary amine catalyst for the asymmetric α-hydroxylation and α-fluorination of α-branched aldehydes is described. The products of the title…”
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Journal Article -
5
Inhibition of ALK2 with bicyclic pyridyllactams
Published in Bioorganic & medicinal chemistry letters (01-01-2022)“…[Display omitted] Activin receptor-like kinase 2 (ALK2) has been implicated as a key target in multiple rare diseases. Herein, we describe the design of a…”
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Journal Article -
6
Catalytic Asymmetric Synthesis of 8-Oxabicyclooctanes by Intermolecular [5+2] Pyrylium Cycloadditions
Published in Angewandte Chemie (02-06-2014)“…Highly enantioselective intermolecular [5+2] cycloadditions of pyrylium ion intermediates with electron‐rich alkenes are promoted by a dual catalyst system…”
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Journal Article -
7
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3
Published in Journal of medicinal chemistry (24-11-2022)“…Upregulation of the fibroblast growth factor receptor (FGFR) signaling pathway has been implicated in multiple cancer types, including cholangiocarcinoma and…”
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Journal Article -
8
X‑ray Characterization and Structure-Based Optimization of Striatal-Enriched Protein Tyrosine Phosphatase Inhibitors
Published in Journal of medicinal chemistry (22-11-2017)“…Excessive activity of striatal-enriched protein tyrosine phosphatase (STEP) in the brain has been detected in numerous neuropsychiatric disorders including…”
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Journal Article -
9
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2
Published in ACS medicinal chemistry letters (14-07-2022)“…Activin receptor-like kinase 2 (ALK2) is a transmembrane kinase receptor that mediates the signaling of the members of the TGF-β superfamily. The aberrant…”
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Journal Article -
10
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach
Published in ACS medicinal chemistry letters (09-03-2023)“…Fibroblast growth factor receptors (FGFRs) are transmembrane receptor tyrosine kinases that regulate multiple physiological processes. Aberrant activation of…”
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Journal Article -
11
Solid phase synthesis of hydrogen bond surrogate derived alpha-helices: resolving the case of a difficult amide coupling
Published in Organic & biomolecular chemistry (21-04-2010)“…Solid phase synthesis of HBS helices involving the Fukuyama-Mitsunobu reaction and triphosgene coupling is described…”
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Journal Article -
12
New meta-terphenyl-derived primary amines in asymmetric catalysis
Published 01-01-2015“…In this dissertation, two distinct asymmetric reaction types are described: [5 + 2] pyrylium cycloadditions and aldehyde ?-functionalizations. Both reactions…”
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Dissertation -
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New meta-terphenyl-derived primary amines in asymmetric catalysis
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Dissertation