Search Results - "Kallemeyn, Jeffrey M."
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Development of an Enantioselective [3 + 2] Cycloaddition To Synthesize the Pyrrolidine Core of ABBV-3221 on Multikilogram Scale
Published in Organic process research & development (15-11-2019)“…The tetrasubstituted pyrrolidine core of ABBV-3221 was synthesized by catalytic, enantioselective cycloaddition. A Cu(I) catalyst system was identified as…”
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Synthesis of 3,4,5-Trisubstituted Isoxazoles via Sequential [3 + 2] Cycloaddition/Silicon-Based Cross-Coupling Reactions
Published in Journal of organic chemistry (01-04-2005)“…A [3 + 2] cycloaddition reaction between alkynyldimethylsilyl ethers and aryl and alkyl nitrile oxides to produce isoxazolylsilanols has been developed. The…”
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Palladium-Catalyzed Silylation of Aryl Bromides Leading to Functionalized Aryldimethylsilanols
Published in Organic letters (18-09-2003)“…A mild and general palladium-catalyzed insertion of 1,2-diethoxy-1,1,2,2-tetramethyldisilane into a variety of aryl bromides affords the aryldimethylsilyl…”
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4
Development of the Enabling Route for Glecaprevir via Ring-Closing Metathesis
Published in Organic process research & development (21-02-2020)“…Glecaprevir was identified as a potent HCV NS3/4A protease inhibitor, and an enabling synthesis was required to support the preclinical evaluation and…”
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5
Stereospecific Palladium-Catalyzed Cross-Coupling of (E)- and (Z)-Alkenylsilanolates with Aryl Chlorides
Published in Journal of the American Chemical Society (20-12-2006)“…The cross-coupling of geometrically defined (E)- and (Z)-alkenyl- and styrylsilanolates with a wide variety of aromatic and heteroaromatic chlorides has been…”
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6
Development of a Large-Scale Route to Glecaprevir: Synthesis of the Macrocycle via Intramolecular Etherification
Published in Organic process research & development (21-08-2020)“…Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale synthesis was required to support the late-stage clinical…”
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A Kinetics-Based Approach for the Assignment of Reactivity Purge Factors
Published in Organic process research & development (20-11-2015)“…The control of mutagenic impurities is of crucial interest to pharmaceutical companies and regulatory agencies alike. One risk-based methodology to assess the…”
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New Semi-Automated Computer-Based System for Assessing the Purge of Mutagenic Impurities
Published in Organic process research & development (15-11-2019)“…The ICH M7 guidance provides a series of flexible control options for the control of (potentially) mutagenic impurities (PMIs) that fully align with key…”
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A consortium-driven framework to guide the implementation of ICH M7 Option 4 control strategies
Published in Regulatory toxicology and pharmacology (01-11-2017)“…The ICH M7 Option 4 control of (potentially) mutagenic impurities is based on the use of scientific principles in lieu of routine analytical testing. This…”
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Scalable Synthesis of a Cis-Substituted Cyclobutyl-Benzothiazole Pyridazinone: Process Development of an Efficient Copper Catalyzed C–N Cross-Coupling Reaction
Published in Organic process research & development (17-01-2014)“…A scalable process for the preparation of 2-(2-(cis-3-(piperidin-1-yl)cyclobutyl)benzothiazol-6-yl)pyridazin-3(2H)-one in multi-kilogram amounts and in high…”
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The Development of Continuous Process for Alkene Ozonolysis Based on Combined in Situ FTIR, Calorimetry, and Computational Chemistry
Published in Organic process research & development (21-01-2011)“…Two continuous apparatuses were designed that are capable of safely scaling the highly energetic ozonolysis reaction to multikilogram scale where flow…”
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Improved Synthesis of 3-Substituted-4-amino-[3,2-c]-thienopyridines
Published in Journal of organic chemistry (15-05-2009)“…Two syntheses of 3-substituted-4-amino-[3,2-c]thienopyridines have been developed to replace the standard literature route to these compounds, which uses…”
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Photochemical Synthesis of 3-Alkynals from 1-Alkynoxy-9,10-anthraquinones
Published in Journal of organic chemistry (15-05-2009)“…Photolysis of 1-(3-alkynoxy)-9,10-anthraquinones in deoxygenated methanol leads to moderate yields (35−45%) of 3-alkynals along with the unexpected formation…”
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Photochemical Synthesis of Aldehydes in the Solid Phase
Published in Journal of organic chemistry (19-04-2002)“…A substituted anthraquinone (AQ), previously shown to photochemically generate benzaldehyde in methanol solution, was attached to a commercially available…”
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Development of a Telescoped Alkylation/Reduction Reaction Sequence and an Asymmetric Hydrogenation to Enable the Kilogram Synthesis of ABBV-3748
Published in Organic process research & development (21-10-2022)“…Challenges in the synthesis of the cystic fibrosis transmembrane receptor corrector ABBV-3748 were addressed to enable a multikilogram-scale GMP sequence…”
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Continuous Process to Safely Manufacture an Aryldiazoacetate and Its Direct Use in a Dirhodium-Catalyzed Enantioselective Cyclopropanation
Published in Organic process research & development (20-01-2023)“…We report the development and demonstration of a continuous-flow process for the safe formation, extraction, and drying of aryldiazoacetate 2, which enables…”
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Establishing Best Practice for the Application and Support of Solubility Purge Factors
Published in Organic process research & development (20-10-2023)“…The increased usage of purge arguments for demonstrating control of mutagenic impurities in drug substances, in accordance with ICH M7, necessitates an…”
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Enhanced Approaches to the Identification, Evaluation, and Control of Impurities
Published in Journal of pharmaceutical innovation (15-06-2019)“…A series of case histories from IQ consortium member companies will be presented to exemplify how the application of the ICH Q11 vision for enhanced or quality…”
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Author Correction: Enhanced Approaches to the Identification, Evaluation, and Control of Impurities
Published in Journal of pharmaceutical innovation (15-06-2019)“…The original version of this article unfortunately contained a mistake. The authors in the author group were listed incorrectly. The correct author group of…”
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The Delivery of Flexibility from the Application of QbD to API Development
Published in Journal of pharmaceutical innovation (01-12-2018)“…This paper by IQ consortium member companies will describe how the application of the ICH Q11 vision for enhanced QbD development can lead to flexibility…”
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