Search Results - "Kolis, Stanley P."
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Process Safety in the Pharmaceutical IndustryPart I: Thermal and Reaction Hazard Evaluation Processes and Techniques
Published in Organic process research & development (20-11-2020)“…Process safety groups in the pharmaceutical industry are important components of active pharmaceutical ingredient (API) development through its life cycle from…”
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Uncovering the Most Kinetically Influential Reaction Pathway Driving the Generation of HCN from Oxyma/DIC Adduct: A Theoretical Study
Published in Industrial & engineering chemistry research (18-01-2023)“…The combination of ethyl (hydroxyimino)cyanoacetate (Oxyma) and diisopropylcarbodiimide (DIC) has demonstrated superior performance in amino acid activation…”
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3
Quantum Mechanical Methods for Thermal Hazard Risk Assessment in Early Phase Pharmaceutical Development
Published in Organic process research & development (21-01-2022)“…Quantum mechanical (QM) applications to predict heat of reaction (ΔH r) and thermal stability of strained aminocarbocylic salts, diazo compounds, and…”
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Generation of Hydrogen Cyanide from the Reaction of Oxyma (Ethyl Cyano(hydroxyimino)acetate) and DIC (Diisopropylcarbodiimide)
Published in Organic process research & development (20-09-2019)“…Evolution of hydrogen cyanide (HCN) during amino acid activation using the reagent combination ethyl cyano(hydroxyimino)acetate…”
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5
Hydrogen Evolution from Telescoped Miyaura Borylation and Suzuki Couplings Utilizing Diboron Reagents: Process Safety and Hazard Considerations
Published in Organic process research & development (18-03-2022)“…The hazard assessment of a telescoped Miyaura borylation and Suzuki coupling reaction employing bis(pinacolato)diboron (BisPin), used in the developmental…”
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Synthesis of Aryl- and Heteroaryl[a]pyrrolo[3,4-c]carbazoles
Published in Journal of organic chemistry (17-10-2003)“…Synthesis of aryl- and hetero[a]pyrrolo[3,4-c]carbazoles by photochemical oxidation and Heck cyclization are described. Photochemical oxidation of 2-naphthyl…”
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Continuous Platform To Generate Nitroalkanes On-Demand (in Situ) Using Peracetic Acid-Mediated Oxidation in a PFA Pipes-in-Series Reactor
Published in Organic process research & development (17-08-2018)“…The synthetic utility of the aza-Henry reaction can be diminished on scale by potential hazards associated with the use of peracid to prepare nitroalkane…”
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Development of an Intermittent-Flow Enantioselective Aza-Henry Reaction Using an Arylnitromethane and Homogeneous Brønsted Acid–Base Catalyst with Recycle
Published in Organic process research & development (19-02-2016)“…A stereoselective aza-Henry reaction between an arylnitromethane and Boc-protected aryl aldimine using a homogeneous Brønsted acid–base catalyst was translated…”
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Synthesis of BACE Inhibitor LY2886721. Part II. Isoxazolidines as Precursors to Chiral Aminothiazines, Selective Peptide Coupling, and a Controlled Reactive Crystallization
Published in Organic process research & development (18-09-2015)“…An efficient synthesis of LY2886721 (1) in five steps and 46% overall yield from the chiral nitrone cycloadduct 2 is presented. Minimizing formation of a…”
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Synthesis of BACE Inhibitor LY2886721. Part I. An Asymmetric Nitrone Cycloaddition Strategy
Published in Organic process research & development (18-09-2015)“…A scalable, asymmetric synthesis of (3aS,6aS)-6a-(5-bromo-2-fluorophenyl)-1-((R)-1-phenylpropyl)tetrahydro-1H,3H-furo[3,4-c]isoxazole, a key intermediate in…”
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(S)-N-{3-[1-Cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: A Potent, Nonsteroidal, Functional Antagonist of the Mineralocorticoid Receptor
Published in Journal of medicinal chemistry (27-12-2007)“…A novel, potent series of indole analogs were recently developed as MR antagonists, culminating in 14. This compound represents the first MR antagonist in this…”
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Development of a Practical Synthesis of an Aminoindanol-Derived M1 Agonist
Published in Organic process research & development (20-03-2009)“…An efficient and scalable synthesis of the clinical candidate 1 is described. The first-generation synthesis built the enantioenriched nitro-aminoindanol core…”
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Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7- a]pyrrolo[3,4- c]carbazoles
Published in Bioorganic & medicinal chemistry letters (21-07-2003)“…The synthesis and CDK inhibitory properties of a series of indolo[6,7- a]pyrrolo[3,4- c]carbazoles is reported. In addition to their potent CDK activity, the…”
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Synthetic Approaches to Indolo[6,7-a]pyrrolo[3,4-c]carbazoles: Potent Cyclin D1/CDK4 Inhibitors
Published in Journal of organic chemistry (30-04-2004)“…Synthesis of indolo[6,7-a]pyrrolo[3,4-c]carbazoles 1, a new class of cyclin D1/CDK4 inhibitors, by oxidation of the corresponding aryl indolylmaleimides 2,…”
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15
Zr-Catalyzed Olefin Alkylations and Allylic Substitution Reactions with Electrophiles
Published in Journal of the American Chemical Society (28-06-2000)“…Disubstituted aryl olefins undergo efficient alkylations in the presence of 5 mol % Cp2ZrCl2, n-BuMgCl, and alkyl tosylates or alkyl bromides. In one class of…”
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Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (02-08-2004)“…The synthesis of a novel series of aza-1,7-annulated indoles is described along with their conversion to indolocarbazoles that proved to be potent kinase…”
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Synthesis of 7-cyano- and 7-acetamido-indoles via cyanocarbonation/hydrogenation of 7-formyl indole
Published in Tetrahedron letters (21-07-2003)“…A procedure for the synthesis of 7-cyano and 7-acetamido indoles via cyanocarbonation/hydrogenation of 7-formyl indole is presented. The process can be…”
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1,7-Annulated indolocarbazoles as cyclin-dependent kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…A series of novel 1,7-annulated indolocarbazoles was prepared and evaluated for kinase inhibitory activity. The synthesis and kinase inhibitory activity of a…”
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Integrating model-based design of experiments and computer-aided solvent design
Published in Computers & chemical engineering (01-09-2023)“…Computer-aided molecular design (CAMD) methods can be used to generate promising solvents with enhanced reaction kinetics, given a reliable model of solvent…”
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Activation of Styrenes toward Diels−Alder Cycloadditions by Osmium(II): Synthesis of Stereodefined Decalin Ring Systems
Published in Journal of the American Chemical Society (18-03-1998)“…The complex [Os(NH3)5(η2-anisole)]2+ reacts with acetals or Michael acceptors to form 4-methoxystyrene complexes that are exclusively coordinated at the arene…”
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