Search Results - "Lee, Ernest E."
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CRTH2 Antagonist MK-7246: A Synthetic Evolution from Discovery through Development
Published in Journal of organic chemistry (02-03-2012)“…In this paper, we report the development of different synthetic routes to MK-7246 (1) designed by the Process Chemistry group. The syntheses were initially…”
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2
Enantioselective Synthesis of Indolizidines Bearing Quaternary Substituted Stereocenters via Rhodium-Catalyzed [2 + 2 + 2] Cycloaddition of Alkenyl Isocyanates and Terminal Alkynes
Published in Organic letters (20-03-2008)“…An enantioselective synthesis of indolizidines bearing quaternary substituted stereocenters by way of a rhodium-catalyzed [2 + 2 + 2] cycloaddition of…”
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3
Total Synthesis of Indolizidine Alkaloid (−)‐209D: Overriding Substrate Bias in the Asymmetric Rhodium‐Catalyzed [2+2+2] Cycloaddition
Published in Angewandte Chemie International Edition (01-01-2009)“…CO! You had me at hello: The use of chiral biphenyl‐based phosphoramidite ligands on rhodium provides an efficient [2+2+2] cycloaddition between terminal alkyl…”
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4
Enantioselective Palladium(II)-Catalyzed Formal [3,3]-Sigmatropic Rearrangement of 2-Allyloxypyridines and Related Heterocycles
Published in Organic letters (15-01-2010)“…Enantioselective palladium(II)-catalyzed formal [3,3]-sigmatropic rearrangement of (E)- and (Z)-allyloxy substituted N-heterocycles generates N-allyl…”
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5
Regioselective rhodium-catalyzed intermolecular [2+2+2] cycloaddition of alkynes and isocyanates to form pyridones
Published in Tetrahedron (27-06-2009)“…A highly regioselective rhodium-catalyzed intermolecular [2+2+2] cycloaddition of terminal alkynes with a variety of isocyanates to provide 2- and 4-pyridones…”
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Journal Article Conference Proceeding -
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Palladium-Catalyzed Allylic Transposition of (Allyloxy) Iminodiazaphospholidines: A Formal [3,3]-Aza-phospha-oxa-Cope Sigmatropic Rearrangement for the Stereoselective Synthesis of Allylic Amines
Published in Journal of the American Chemical Society (26-10-2005)“…The synthesis of N-protected allylic amines has been achieved utilizing a palladium(II)-catalyzed, [3,3]-rearrangement of (allyloxy) iminodiazaphospholidines…”
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Enantioselective Rhodium-Catalyzed [2 + 2 + 2] Cycloadditions of Terminal Alkynes and Alkenyl Isocyanates: Mechanistic Insights Lead to a Unified Model that Rationalizes Product Selectivity
Published in Journal of the American Chemical Society (04-11-2009)“…This manuscript describes the development and scope of the asymmetric rhodium-catalyzed [2 + 2 + 2] cycloaddition of terminal alkynes and alkenyl isocyanates…”
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8
Diastereoselective synthesis of fluorinated piperidine quinazoline spirocycles as iNOS selective inhibitors
Published in Tetrahedron letters (13-06-2012)“…A diastereoselective synthesis of fluoropiperidine quinazoline spirocycles has been developed through a silyl triflate mediated intermolecular coupling of…”
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9
Effect of acid catalysis on the direct electrophilic fluorination of ketones, ketals, and enamides using Selectfluor
Published in Tetrahedron letters (13-06-2012)“…The fluorination of ketones, ketals, and enamides has been achieved using the electrophilic fluorinating reagent Selectfluor™ (F-TEDA-BF4). For the reactions…”
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Journal Article -
10
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two…”
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11
Effect of ethnicity on the risk of developing nonmelanoma skin cancer following long-term PUVA therapy
Published in International journal of dermatology (01-12-2005)“…Background Research demonstrating an increased incidence of skin cancer with psoralen plus ultraviolet A (PUVA) therapy has reflected the Caucasian…”
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Journal Article -
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Palladium-Catalyzed [3,3] Sigmatropic Rearrangement of (Allyloxy)iminodiazaphospholidines: Allylic Transposition of CO and CN Functionality
Published in Angewandte Chemie International Edition (26-03-2004)“…A PVN to PVO interconversion is the thermodynamic driving force for the title reaction. Iminodiazaphospholidines 1 give phosphoramides 2, which are…”
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13
Is contact allergy in man lifelong? An overview of patch test follow-ups
Published in Contact dermatitis (01-03-2001)“…In contradistinction from certain strains of mice, contact allergy in man is hypothesized to be either lifelong or at least to last for years. We examined…”
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Journal Article -
14
Synthesis of oligosaccharide fragments of the glycosylinositolphospholipid of Trypanosoma cruzi: a new selenoglycoside glycosyl donor for the preparation of 4-thiogalactofuranosyl analogues
Published in Tetrahedron: asymmetry (28-01-2000)“…A new selenoglycoside, phenyl 2,3,5,6-tetra- O-acetyl-4-thio-1-selenogalactofuranose, has been synthesized. This 4-thiogalactofuranosyl donor was used in the…”
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Journal Article -
15
Effect of acid catalysis on the direct electrophilic fluorination of ketones, ketals, and enamides using Selectfluorac
Published in Tetrahedron letters (13-06-2012)“…The fluorination of ketones, ketals, and enamides has been achieved using the electrophilic fluorinating reagent Selectfluorac (F-TEDA-BF4). For the reactions…”
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Journal Article -
16
Discovery of Mix-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
Published in Bioorganic & medicinal chemistry letters (2011)Get full text
Journal Article -
17
Treatment of urticaria. An evidence-based evaluation of antihistamines
Published in American journal of clinical dermatology (2001)“…Urticaria is a cutaneous syndrome characterized by dermal edema (wheal) and erythema (flare) that blanches with pressure. The lesions typically last less than…”
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Journal Article -
18
Total Synthesis of Indolizidine Alkaloid (−)‐209D: Overriding Substrate Bias in the Asymmetric Rhodium‐Catalyzed [2+2+2] Cycloaddition
Published in Angewandte Chemie (16-03-2009)“…CO auf Wanderschaft: Mit chiralen Biphenyl‐basierten Phosphoramiditliganden an Rhodium lässt sich eine effiziente [2+2+2]‐Cycloaddition zwischen endständigen…”
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Journal Article -
19
Is contact allergy in man lifelong?
Published in Contact dermatitis (01-03-2001)“…In contradistinction from certain strains of mice, contact allergy in man is hypothesized to be either lifelong or at least to last for years. We examined…”
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Journal Article -
20
Palladium-Catalyzed [3,3] Sigmatropic Rearrangement of (Allyloxy)iminodiazaphospholidines: Allylic Transposition of CO and CN Functionality
Published in Angewandte Chemie (26-03-2004)“…Die thermodynamische Triebkraft der Titelreaktion ist die Umwandlung einer PVN‐ in eine PVO‐Gruppe: Iminodiazaphospholidine 1 liefern Phosphorsäuretriamide…”
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