Search Results - "Pietz, Mark A"
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Development of a Leuckart–Wallach Reaction in Flow for the Synthesis of Abemaciclib
Published in Organic process research & development (15-09-2017)“…The development of a route for a key building block in the synthesis of abemaciclib is described. The route proceeds through a Leuckart–Wallach reductive…”
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Use of Modeling and Process Analytical Technologies in the Design of a Catalytic Amination Reaction: Understanding Oxygen Sensitivity at the Lab and Manufacturing Scales
Published in Organic process research & development (17-01-2014)“…A mechanistic approach was undertaken to understand the oxygen sensitivity of a Pd-catalyzed amination reaction used in the synthesis of an active…”
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Development of an Improved Route for the Synthesis of an Abemaciclib Intermediate
Published in Organic process research & development (15-11-2019)“…A new synthesis for an intermediate of abemaciclib is described. Keys to this route are the use of inexpensive starting materials, biphasic amine alkylation…”
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Mitigating the Risk of Coprecipitation of Pinacol during Isolation from Telescoped Miyaura Borylation and Suzuki Couplings Utilizing Boron Pinacol Esters: Use of Modeling for Process Design
Published in Organic process research & development (19-02-2016)“…Process definition and optimization of a telescoped Miyaura borylation and Suzuki coupling reaction employing bis(pinacolato)diboron (BisPin), used in the…”
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Practical Asymmetric Synthesis of an Edivoxetine·HCl Intermediate via an Efficient Diazotization Process
Published in Organic process research & development (17-04-2015)“…A convergent synthesis of (S)-(4-benzylmorpholin-2-yl)(morpholino)methanone methanesulfonate (1), a key regulatory starting material for edivoxetine·HCl, was…”
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Practical Synthesis of Chiral 2-Morpholine: (4-Benzylmorpholin-2-(S)-yl)-(tetrahydropyran-4-yl)methanone Mesylate, a Useful Pharmaceutical Intermediate
Published in Organic process research & development (20-03-2009)“…A commercial synthesis was developed for the production of (4-benzylmorpholin-2-(S)-yl)-(tetrahydropyran-4-yl)methanone mesylate, 1a, a key starting material…”
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Identifying Scale Sensitivity for API Crystallizations from Desupersaturation Measurements
Published in Organic process research & development (20-03-2009)“…The present report details a methodology for discriminating between mass transfer- and surface integration-controlled crystallizations. Initial…”
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Pilot-Plant Preparation of an αvβ3 Integrin Antagonist. Part 3. Process Research and Development of a Diisopropylcarbodiimide and Catalytic 1-Hydroxybenzotriazole Peptide Coupling
Published in Organic process research & development (20-11-2009)“…Studies directed toward the process research, development, and scale-up preparation of the potential αvβ3 integrin antagonist 1 are described. A convergent…”
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Pilot-Plant Preparation of an α v β 3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling
Published in Organic process research & development (16-01-2009)Get full text
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Pilot-Plant Preparation of an αvβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling
Published in Organic process research & development (16-01-2009)“…The process development of a peptide coupling with CDI is discussed. Various solvents, addition orders, stoichiometries, and reaction temperatures were…”
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