Search Results - "Kiesman, William F"

Development of Kilogram-Scale Convergent Liquid-Phase Synthesis of Oligonucleotides by Zhou, Xuan, Kiesman, William F, Yan, Wuming, Jiang, Hong, Antia, Firoz D, Yang, Jing, Fillon, Yannick A, Xiao, Li, Shi, Xianglin

“…Oligonucleotide drugs show promise to treat diseases afflicting millions of people. To address the need to manufacture large quantities of oligonucleotide…”
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The Chelate Effect Rationalizes Observed Rate Acceleration and Enantioselectivity in BINOL‐Catalyzed Petasis Reactions by Haeffner, Fredrik, Pickel, Thomas C., Hou, April, Walker, Donald G., Kiesman, William F., Shi, Xianglin

“…Density functional theory (DFT) calculations afforded insight into the origin of the experimentally observed reaction rate acceleration (≥500 fold) and…”
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A1 adenosine receptor antagonists, agonists, and allosteric enhancers by Kiesman, William F, Elzein, Elfatih, Zablocki, Jeff

“…Intense efforts of many pharmaceutical companies and academicians in the A(1) adenosine receptor (AR) field have led to the discovery of clinical candidates…”
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Solid-Phase Synthesis of Phosphorothioate Oligonucleotides Using Sulfurization Byproducts for in Situ Capping by Yang, Jimin, Stolee, Jessica A, Jiang, Hong, Xiao, Li, Kiesman, William F, Antia, Firoz D, Fillon, Yannick A, Ng, Austen, Shi, Xianglin

“…Oligonucleotides containing phosphorothioate (PS) linkages have recently demonstrated significant clinical utility. PS oligonucleotides are manufactured via a…”
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Catalytic Asymmetric Petasis Reactions of Vinylboronates by Shi, Xianglin, Kiesman, William F, Levina, Anna, Xin, Zhili

“…Binaphthol-catalyzed asymmetric Petasis reactions of salicylaldehydes with dibutyl vinylboronates and secondary amines in the presence of 4 Å molecular sieves…”
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Synthesis of Vixotrigine, a Voltage- and Use-Dependent Sodium Channel Blocker. Part 2: Development of a Late-Stage Process by Chen, Robbie, Couming, Vincent, Guzowski, John, Irdam, Erwin, Kiesman, William F, Kwok, Daw-Iong Albert, Liang, Wenli, Mack, Tamera, O’Brien, Erin M, Opalka, Suzanne M, Patience, Daniel, Sahli, Stefan, Walker, Donald G, Osei-Yeboah, Frederick, Gu, Chaozhan, Zhang, Xin, Stöckli, Markus, Stucki, Thiemo, Matzinger, Hanspeter, Kuhn, Roman, Thut, Michael, Grohmann, Markus, Haefner, Benjamin, Lotz, Joerg, Nonnenmacher, Michael, Cerea, Paolangelo

“…As vixotrigine (1) entered a later clinical phase for trigeminal neuralgia ( Zakrzewska, J. M. ; et al. Lancet Neurol. 2017, 16, 291−300 ), the development of…”
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Acceleration of Petasis Reactions of Salicylaldehyde Derivatives with Molecular Sieves by Shi, Xianglin, Hebrault, Dominique, Humora, Michael, Kiesman, William F, Peng, Hairuo, Talreja, Tina, Wang, Zezhou, Xin, Zhili

“…Mild reaction conditions for Petasis reactions of substituted salicylaldehydes with various amines and arylboronic acids in the presence of molecular sieves…”
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Process Development of an N‑Benzylated Chloropurine at the Kilogram Scale by Shi, Xianglin, Chang, Hexi, Grohmann, Markus, Kiesman, William F, Kwok, Daw-Iong Albert

“…A two-step pharmaceutical manufacturing process was developed for the large-scale preparation of…”
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Tricyclic Imidazoline Derivatives as Potent and Selective Adenosine A1 Receptor Antagonists by Vu, Chi B, Kiesman, William F, Conlon, Patrick R, Lin, Ko-Chung, Tam, Melissa, Petter, Russell C, Smits, Glenn, Lutterodt, Frank, Jin, Xiaowei, Chen, Liqing, Zhang, Jianbo

“…Novel tricyclic imidazoline antagonists of the adenosine A1 receptor are described. For key compounds, the selectivity level over other adenosine receptor…”
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Case Studies in the Applicability of Drug Substance Design Spaces Developed on the Laboratory Scale to Commercial Manufacturing by Thomson, Nicholas M, Seibert, Kevin D, Tummala, Srinivas, Bordawekar, Shailendra, Kiesman, William F, Irdam, Erwin A, Phenix, Brian, Kumke, Daniel

“…A number of strategies have been employed within the pharmaceutical industry in order to mitigate the risk of applying design space boundaries developed on the…”
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Case Studies in the Development of Drug Substance Control Strategies by Thomson, Nicholas M, Singer, Robert, Seibert, Kevin D, Luciani, Carla V, Srivastava, Sushil, Kiesman, William F, Irdam, Erwin A, Lepore, John V, Schenck, Luke

“…A series of case histories from IQ consortium member companies are presented in order to exemplify many of the different elements of drug substance control…”
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Part 1: A Review and Perspective of the Regulatory Guidance to Support Designation and Justification of API Starting Material by Faul, Margaret M, Kiesman, William F, Smulkowski, Maciej, Pfeiffer, Steven, Busacca, Carl A, Eriksson, Magnus C, Hicks, Fred, Orr, John D

“…Designation and justification of active pharmaceutical ingredient starting material (API SM) is a standard part of the drug substance (DS) development and…”
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Part 2: Designation and Justification of API Starting Materials: Current Practices across Member Companies of the IQ Consortium by Faul, Margaret M, Busacca, Carl A, Eriksson, Magnus C, Hicks, Fred, Kiesman, William F, Smulkowski, Maciej, Orr, John D, Pfeiffer, Steven

“…Designation and justification of active pharmaceutical ingredient starting material (API SM) is a standard part of the drug development and commercialization…”
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Part 3: Designation and Justification of API Starting Materials: Proposed Framework for Alignment from an Industry Perspective by Faul, Margaret M, Argentine, Mark D, Egan, Marjorie, Eriksson, Magnus C, Ge, Zhihong, Hicks, Fred, Kiesman, William F, Mergelsberg, Ingrid, Orr, John D, Smulkowski, Maciej, Wächter, Gerald A

“…Designation and justification of an Active Pharmaceutical Ingredient Starting Material (API SM) is an important aspect of the drug development and…”
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Detection of Aryl Radicals in Hydrodediazoniations by Wassmundt, Frederick W, Kiesman, William F

“…Iodoacetic acid, an effective aryl radical trapping agent, was employed to investigate the reactive intermediates in several hydrodediazoniations. Isolation of…”
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Synthesis of alkyne derivatives of a novel triazolopyrazine as A2A adenosine receptor antagonists by YAO, Gang, HAQUE, Serajul, PETTER, Russell C, LI SHA, KUMARAVEL, Gnanasambandam, WANG, Joy, ENGBER, Thomas M, WHALLEY, Eric T, CONLON, Patrick R, HEXI CHANG, KIESMAN, William F

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Soluble Catalysts for Improved Pschorr Cyclizations by Wassmundt, Frederick W, Kiesman, William F

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Understanding and Control of Dimethyl Sulfate in a Manufacturing Process: Kinetic Modeling of a Fischer Esterification Catalyzed by H2SO4 by Guzowski, John P, Delaney, Edward J, Humora, Michael J, Irdam, Erwin, Kiesman, William F, Kwok, Albert, Moran, Amy D

“…The formation and fate of monomethyl sulfate (MMS) and dimethyl sulfate (DMS) were studied by proton NMR for a sulfuric acid catalyzed esterification reaction…”
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Potent and Orally Bioavailable 8-Bicyclo[2.2.2]octylxanthines as Adenosine A1 Receptor Antagonists by Kiesman, William F, Zhao, Jin, Conlon, Patrick R, Dowling, James E, Petter, Russell C, Lutterodt, Frank, Jin, Xiaowei, Smits, Glenn, Fure, Mary, Jayaraj, Andrew, Kim, John, Sullivan, Gail, Linden, Joel

“…In the search for a selective adenosine A1 receptor antagonist with greater aqueous solubility than the compounds currently in clinical trials as diuretics, a…”
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Highly Regio- and Enantioselective Catalytic Hydrogenation of Enamides in Conjugated Diene Systems:  Synthesis and Application of γ,δ-Unsaturated Amino Acids by Burk, Mark J, Allen, John G, Kiesman, William F

“…An extremely efficient method has been found for the catalytic asymmetric hydrogenation of conjugated α,γ-dienamide esters using the Et-DuPHOS-Rh catalyst…”
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