Search Results - "Conlon, David A."

Development of a Practical Synthesis of Functionalized Azaxanthene-Derived Nonsteroidal Glucocorticoid Receptor Modulators by Conlon, David A, Natalie, Kenneth J, Cuniere, Nicolas, Razler, Thomas M, Zhu, Jason, de Mas, Nuria, Tymonko, Steven, Fraunhoffer, Kenneth J, Sortore, Eric, Rosso, Victor W, Xu, Zhongmin, Adams, Monica L, Patel, Anisha, Huang, Jun, Gong, Hua, Weinstein, David S, Quiroz, Fernando, Chen, Doris C

“…An efficient route to two functionalized 2-aryl-5H-chromeno­[2,3-b]­pyridines (azaxanthenes) is reported. The addition of lithiated 2,6-dichloropyridine to…”
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Development of a Practical Synthesis of a Functionalized Pyrrolo[2,1-f][1,2,4]triazine Nucleus by Zheng, Bin, Conlon, David A, Corbett, R. Michael, Chau, Melissa, Hsieh, Dau-Ming, Yeboah, Agnes, Hsieh, Daniel, Müslehiddinoğlu, Jale, Gallagher, William P, Simon, Jeffrey N, Burt, Justin

“…Functionalized pyrrolotriazine 1b is a key heterocyclic building block in the synthesis of BMS-690514, a potent anticancer agent. Described herein are our…”
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Inhibitors of HIV‑1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir by Meanwell, Nicholas A, Krystal, Mark R, Nowicka-Sans, Beata, Langley, David R, Conlon, David A, Eastgate, Martin D, Grasela, Dennis M, Timmins, Peter, Wang, Tao, Kadow, John F

“…Human immunodeficiency virus-1 (HIV-1) infection currently requires lifelong therapy with drugs that are used in combination to control viremia. The…”
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Catalytic syn-Selective Direct Aldol Reactions of Benzophenone Glycine Imine with Aromatic, Heteroaromatic and Aliphatic Aldehydes by Lou, Sha, Ramirez, Antonio, Conlon, David A.

“…We have developed highly diastereoselective silver‐catalyzed direct aldol reactions of benzophenone glycine imines with aromatic, heteroaromatic and aliphatic…”
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Considerations for Starting Material Designation for Drug-Linkers in Antibody–Drug Conjugates by Jones, Michael T., Dirat, Olivier, Conlon, David A., Melucci, Charles, Schrier, Kate, Raglione, Thomas, Zhang, Qunying, Bulger, Paul G.

“…By combining the unique targeting ability of monoclonal antibodies with the cancer-killing ability of cytotoxins, antibody–drug conjugates (ADCs) exhibit…”
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Development of a Scalable Route to a Dual NK-1/Serotonin Receptor Antagonist by Risatti, Christina, Natalie, Kenneth J, Shi, Zhongping, Conlon, David A

“…The evolution of a process for the preparation of a new heterocyclic dual NK1/serotonin receptor antagonist is described. The final synthesis features a…”
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Synthesis of the 6‑Azaindole Containing HIV‑1 Attachment Inhibitor Pro-Drug, BMS-663068 by Chen, Ke, Risatti, Christina, Bultman, Michael, Soumeillant, Maxime, Simpson, James, Zheng, Bin, Fanfair, Dayne, Mahoney, Michelle, Mudryk, Boguslaw, Fox, Richard J, Hsaio, Yi, Murugesan, Saravanababu, Conlon, David A, Buono, Frederic G, Eastgate, Martin D

“…The development of a short and efficient synthesis of a complex 6-azaindole, BMS-663068, is described. Construction of the 6-azaindole core is quickly…”
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Syn-Selective Synthesis of β‑Branched α‑Amino Acids by Alkylation of Glycine-Derived Imines with Secondary Sulfonates by Lou, Sha, McKenna, Grace M, Tymonko, Steven A, Ramirez, Antonio, Benkovics, Tamas, Conlon, David A, González-Bobes, Francisco

“…A syn-selective synthesis of β-branched α-amino acids has been developed based on the alkylation of glycine imine esters with secondary sulfonates. The…”
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Asymmetric Synthesis of a Potent, Aminopiperidine-Fused Imidazopyridine Dipeptidyl Peptidase IV Inhibitor by Xu, Feng, Corley, Edward, Zacuto, Michael, Conlon, David A, Pipik, Brenda, Humphrey, Guy, Murry, Jerry, Tschaen, David

“…A practical asymmetric synthesis of a novel aminopiperidine-fused imidazopyridine dipeptidyl peptidase IV (DPP-4) inhibitor 1 has been developed. Application…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 7. Development of a Regioselective Ullmann–Goldberg–Buchwald Reaction by Gallagher, William P, Soumeillant, Maxime, Chen, Ke, Fox, Richard J, Hsiao, Yi, Mack, Brendan, Iyer, Vidya, Fan, Junying, Zhu, Jason, Beutner, Gregory, Silverman, Steven M, Fanfair, Dayne D, Glace, Andrew W, Freitag, Adam, Sweeney, Jason, Ji, Yining, Blackmond, Donna G, Eastgate, Martin D, Conlon, David A

“…The discovery, development, and optimization of an Ullmann–Goldberg–Buchwald coupling reaction is described. This complex process represents a key…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 5. Selective C‑7 Bromination of the 6‑Azaindole Core by González-Bobes, Francisco, Hickey, Matthew R, Cohen, Benjamin, Bultman, Michael, Chen, Ke, Fanfair, Dayne, Rosso, Victor W, Strotman, Neil A, Mudryk, Boguslaw, Murugesan, Saravanababu, Schild, Richard L, Ivy, Sabrina, Eastgate, Martin D, Sweeney, Jason T, Conlon, David A

“…We report research focused on the preparation of an advanced intermediate in the synthesis of a novel antiretroviral. This manuscript describes the development…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 2. Strategic Selections in the Transition from an Enabling Route to a Commercial Synthesis by Chen, Ke, Risatti, Christina, Simpson, James, Soumeillant, Maxime, Soltani, Michelle, Bultman, Michael, Zheng, Bin, Mudryk, Boguslaw, Tripp, Jonathan C, La Cruz, Thomas E, Hsiao, Yi, Conlon, David A, Eastgate, Martin D

“…During the process of developing a synthesis to a complex molecule, multiple decisions are made regarding the strategies and tactics used to prepare key bonds…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 3. Mechanistic Studies Enable a Scale-Independent Friedel–Crafts Acylation by Beutner, Gregory L, Albrecht, Jacob, Fan, Junying, Fanfair, Dayne, Lawler, Michael J, Bultman, Michael, Chen, Ke, Ivy, Sabrina, Schild, Richard L, Tripp, Jonathan C, Murugesan, Saravanababu, Dambalas, Konstantinos, McLeod, Douglas D, Sweeney, Jason T, Eastgate, Martin D, Conlon, David A

“…During the development of a Friedel–Crafts acylation for the preparation of a key pyrrole intermediate in the synthesis of the HIV attachment inhibitor,…”
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A Partial Classical Resolution/Preparative Chiral Supercritical Fluid Chromatography Method for the Rapid Preparation of the Pivotal Intermediate in the Synthesis of Two Nonsteroidal Glucocorticoid Receptor Modulators by de Mas, Nuria, Natalie, Kenneth J, Quiroz, Fernando, Rosso, Victor W, Chen, Doris C, Conlon, David A

“…Preparative chiral supercritical fluid chromatography (SFC) employing an enantioenriched feedstock obtained via partial classical resolution enabled rapid…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 6. Friedel–Crafts Acylation/Hydrolysis and Amidation by Zheng, Bin, Silverman, Steven M, Steinhardt, Sarah E, Kolotuchin, Sergei, Iyer, Vidya, Fan, Junying, Skliar, Dimitri, McLeod, Douglas D, Bultman, Michael, Tripp, Jonathan C, Murugesan, Saravanababu, La Cruz, Thomas E, Sweeney, Jason T, Eastgate, Martin D, Conlon, David A

“…The development of a process for appending the oxalyl amide side chain to the azaindole core of the HIV-attachment inhibitor BMS-663068 is described. A…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 1. Evolution of Enabling Strategies by Fox, Richard J, Tripp, Jonathan C, Schultz, Mitchell J, Payack, Joseph F, Fanfair, Dayne D, Mudryk, Boguslaw M, Murugesan, Saravanababu, Chen, Chung-Pin H, La Cruz, Thomas E, Ivy, Sabrina E, Broxer, Sévrine, Cullen, Ryan, Erdemir, Deniz, Geng, Peng, Xu, Zhongmin, Fritz, Alan, Doubleday, Wendel W, Conlon, David A

“…The development of two enabling routes that led to the production of >1000 kg of BMS-663068 (3) is described. The route identified for the initial 100 kg…”
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Development of a New and Practical Route to Chiral 3,4-Disubstituted Cyclopentanones:  Asymmetric Alkylation and Intramolecular Cyclopropanation as Key C−C Bond-Forming Steps by Palucki, Michael, Um, Joann M, Yasuda, Nobuyoshi, Conlon, David A, Tsay, Fuh-Rong, Hartner, Frederick W, Hsiao, Yi, Marcune, Benjamin, Karady, Sandor, Hughes, David L, Dormer, Peter G, Reider, Paul J

“…An efficient and practical asymmetric synthesis of (+)-trans-3-hydroxymethyl-4-(3-fluorophenyl)cyclopentanone (1) is described. An asymmetric Mo-catalyzed…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 4. Synthesis of the 6‑Azaindole Core by Bultman, Michael S, Fan, Junying, Fanfair, Dayne, Soltani, Michelle, Simpson, James, Murugesan, Saravanababu, Soumeillant, Maxime, Chen, Ke, Risatti, Christina, La Cruz, Thomas E, Buono, Frederic G, Hung, Victor, Schild, Richard L, Ivy, Sabrina, Sweeney, Jason T, Conlon, David A, Eastgate, Martin D

“…We report research focused on the construction of the 6-azaindole core, a key intermediate in the synthesis of the clinical candidate BMS-663068. The work…”
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Development of a Process for the Preparation of Chloromethyl Chlorosulfate by Zheng, Bin, Sugiyama, Masano, Eastgate, Martin D, Fritz, Alan, Murugesan, Saravanababu, Conlon, David A

“…A new and efficient synthesis of chloromethyl chlorosulfate (CMCS) from chloroiodomethane and chlorosulfonic acid is described. This process leverages a…”
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Translating evidence-based practice: safe and accurate blood pressure measurement in a comprehensive cancer center by Conlon, David A

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