Search Results - "KOSJEK, Birgit"
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Advances in the Enzymatic Reduction of Ketones
Published in Accounts of chemical research (01-12-2007)“…Historically, biocatalytic ketone reductions involved the use of Bakerʼs yeast. Within the last five years, a significant and growing number of isolated…”
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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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3
Green and sustainable metrics: Charting the course for green-by-design small molecule API synthesis
Published in Current research in green and sustainable chemistry (2022)“…Sustainable small molecule Active Pharmaceutical Ingredient (API) manufacturing starts at the onset of route development by employing a Green-by-Design…”
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Biocatalytic Asymmetric Hydrogen Transfer Employing Rhodococcus ruber DSM 44541
Published in Journal of organic chemistry (24-01-2003)“…Nonracemic sec-alcohols of opposite absolute configuration were obtained either by asymmetric reduction of the corresponding ketone using 2-propanol as…”
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5
Purification and characterization of a chemotolerant alcohol dehydrogenase applicable to coupled redox reactions
Published in Biotechnology and bioengineering (05-04-2004)“…The purification and characterization of an organic solvent tolerant, NADH‐dependent medium‐chain secondary alcohol dehydrogenase (denoted sec‐ADH “A”) from…”
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Non-Racemic Halohydrins via Biocatalytic Hydrogen-Transfer Reduction of Halo-Ketones and One-Pot Cascade Reaction to Enantiopure Epoxides
Published in Advanced synthesis & catalysis (01-11-2005)“…Biocatalytic hydrogen‐transfer reduction of α‐chloro‐ketones furnished non‐racemic chlorohydrins by employing either Rhodococcus ruber as lyophilized cell…”
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7
Recent preparative applications of redox enzymes
Published in Current opinion in chemical biology (01-04-2019)“…Redox enzymes offer many powerful transformations for the efficient industrial-scale synthesis of diverse chemicals desired by society. Here we survey recent…”
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Biocatalytic oxidative kinetic resolution of sec-alcohols: stereocontrol through substrate-modification
Published in Tetrahedron: asymmetry (01-01-2003)“…Whole lyophilised cells of Rhodococcus ruber DSM 44541 were employed for the oxidative kinetic resolution of sec-alcohols using acetone as hydrogen acceptor…”
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Selective Synthesis of N 6,3′,5′-Tripivaloyladenosine via Dynamic Kinetic Crystallization and Regioselective Preparation of Pivalated 2′-Deoxy-2′-fluoroarabinoadenosines
Published in Organic process research & development (15-11-2024)“…A four chemical step route to 2′-deoxy-2′-fluoro-N 6,3′-dipivaloylarabinoadenosine and 2′-deoxy-2′-fluoro-N 6-pivaloylarabinoadenosine from adenosine was…”
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Driving Aspirational Process Mass Intensity Using Simple Structure-Based Prediction
Published in Organic process research & development (20-05-2022)“…An important metric for gauging the impact that a synthetic route has on chemical resources, cost, and sustainability is process mass intensity (PMI)…”
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Resolution of 2,2-Disubstituted Epoxides via Biocatalytic Azidolysis
Published in Organic letters (03-09-2010)“…A practical procedure for the enzymatic resolution of 2-alkyl-2-aryl-disubstituted epoxides using the Codex HHDH P2E2 enzyme and sodium azide is reported. This…”
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Evolution of a Green and Sustainable Manufacturing Process for Belzutifan: Part 1Process History and Development Strategy
Published in Organic process research & development (16-02-2024)“…An improved synthesis has been developed for belzutifan, a novel HIF-2α inhibitor for the treatment of Von Hippel–Lindau (VHL) disease-associated renal cell…”
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Improved iGAL 2.0 Metric Empowers Pharmaceutical Scientists to Make Meaningful Contributions to United Nations Sustainable Development Goal 12
Published in ACS sustainable chemistry & engineering (25-04-2022)“…The large and steadily growing demand for medicines combined with their inherent resource-intensive manufacturing necessitates a relentless push for their…”
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Evolution of a Green and Sustainable Manufacturing Process for Belzutifan: Part 5Chemoenzymatic Diastereoselective Fluorination/DKR
Published in Organic process research & development (16-02-2024)“…A ketone fluorination/reduction dynamic kinetic resolution (DKR) was developed for a third-generation synthesis of belzutifan. This new process replaced a…”
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Harnessing the Power of Catalysis for the Synthesis of CRTH2 Antagonist MK-1029
Published in Organic process research & development (18-03-2022)“…The synthetic strategy utilized to prepare clinical supplies of CRTH2 antagonist MK-1029 is described. Specifically, the approach communicated is predicated on…”
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Scalable Asymmetric Synthesis of MK-8998, a T‑Type Calcium Channel Antagonist
Published in Journal of organic chemistry (18-02-2022)“…Two scalable and efficient synthetic routes for the synthesis of a T-type calcium channel antagonist MK-8998 were developed from a simple pyridine building…”
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Process Development of C–N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib
Published in Organic process research & development (17-01-2014)“…Process development of the synthesis of the orally active poly(ADP-ribose)polymerase inhibitor niraparib is described. Two new asymmetric routes are reported,…”
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Engineering Hydroxylase Activity, Selectivity, and Stability for a Scalable Concise Synthesis of a Key Intermediate to Belzutifan
Published in Angewandte Chemie International Edition (22-03-2024)“…Biocatalytic oxidations are an emerging technology for selective C−H bond activation. While promising for a range of selective oxidations, practical use of…”
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Synthesis of Vibegron Enabled by a Ketoreductase Rationally Designed for High pH Dynamic Kinetic Reduction
Published in Angewandte Chemie International Edition (04-06-2018)“…Described here is an efficient stereoselective synthesis of vibegron enabled by an enzymatic dynamic kinetic reduction that proceeds in a high‐pH environment…”
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MISER chromatography (multiple injections in a single experimental run): the chromatogram is the graph
Published in Tetrahedron: asymmetry (2010)“…An experimental approach for rapid analysis and convenient interpretation of multiparallel experiments is described. Conventional approaches use a series of…”
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