8 research outputs found
Asymmetric Synthesis of Substituted 2-Azaspiro[3.5]nonan-1-ones: An Enantioselective Synthesis of the Cholesterol Absorption Inhibitor (+)-SCH 54016
No full textEnzymatic Desymmetrization of Prochiral 2-Substituted-1,3-propanediols: A Practical Chemoenzymatic Synthesis of a Key Precursor of SCH51048, a Broad-Spectrum Orally Active Antifungal Agent
No full textPilot-Scale Lipase-Catalyzed Regioselective Acylation of Ribavirin in Anhydrous Media in the Synthesis of a Novel Prodrug Intermediate
No full textPreparative regioselective acylation of glycols by enzymatic transesterification in organic solvents
No full textEfficient, Chemoenzymatic Process for Manufacture of the Boceprevir Bicyclic [3.1.0]Proline Intermediate Based on Amine Oxidase-Catalyzed Desymmetrization
No full textThe key structural feature in Boceprevir, Merck’s
new drug
treatment for hepatitis C, is the bicyclic [3.1.0]proline moiety “P2”.
During the discovery and development stages, the P2 fragment was produced
by a classical resolution approach. As the drug candidate advanced
through clinical trials and approached regulatory approval and commercialization,
Codexis and Schering–Plough (now Merck) jointly developed a
chemoenzymatic asymmetric synthesis of P2 where the net reaction was
an oxidative Strecker reaction. The key part of this reaction sequence
is an enzymatic oxidative desymmetrization of the prochiral amine
substrate
Abstracts of The Second Eurasian RISK-2020 Conference and Symposium
No full textThis abstract book contains abstracts of the various research ideas presented at The Second Eurasian RISK-2020 Conference and Symposium.The RISK-2020 Conference and Symposium served as a perfect venue for practitioners, engineers, researchers, scientists, managers and decision-makers from all over the world to exchange ideas and technology about the latest innovation developments dealing with risk minimization
