Search Results - "Buzon, Richard"

Syntheses of 4,5-Disubstituted Oxazoles via Regioselective C-4 Bromination by Li, Bryan, Buzon, Richard A, Zhang, Zhijun

“…A scaleable and highly regioselective C-4 bromination of 5-substituted oxazoles is described. The use of DMF as solvent played a critical role in significantly…”
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Aqueous Phosphoric Acid as a Mild Reagent for Deprotection of tert-Butyl Carbamates, Esters, and Ethers by Li, Bryan, Berliner, Martin, Buzon, Richard, Chiu, Charles K.-F, Colgan, Stephen T, Kaneko, Takushi, Keene, Nandell, Kissel, William, Le, Tung, Leeman, Kyle R, Marquez, Brian, Morris, Ronald, Newell, Lisa, Wunderwald, Silke, Witt, Michael, Weaver, John, Zhang, Zhijun, Zhang, Zhongli

“…Aqueous phosphoric acid (85 wt %) is an effective, environmentally benign reagent for the deprotection of tert-butyl carbamates, tert-butyl esters, and…”
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An Asymmetric Synthesis of (2S,5S)-5-Substituted Azepane-2-Carboxylate Derivatives by Wishka, Donn G, Bédard, Marion, Brighty, Katherine E, Buzon, Richard A, Farley, Kathleen A, Fichtner, Michael W, Kauffman, Goss S, Kooistra, Jaap, Lewis, Jason G, O’Dowd, Hardwin, Samardjiev, Ivan J, Samas, Brian, Yalamanchi, Geeta, Noe, Mark C

“…To facilitate a drug discovery project, we needed to develop a robust asymmetric synthesis of (2S,5S)-5-substituted-azepane-2-carboxylate derivatives. Two key…”
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Process Development of a Novel Azetidinyl Ketolide Antibiotic by Li, Bryan, Magee, Thomas V, Buzon, Richard A, Widlicka, Daniel W, Bill, Dave R, Brandt, Thomas, Cao, Xiaoping, Coutant, Michael, Dou, Haijian, Granskog, Karl, Flanagan, Mark E, Hayward, Cheryl M, Li, Bin, Liu, Fengwei, Liu, Wei, Nguyen, Thuy-Trinh, Raggon, Jeffrey W, Rose, Peter, Rainville, Joseph, Reilly, Usa Datta, Shen, Yue, Sun, Jianmin, Wilcox, Glenn E

“…Process development and the multikilogram synthesis of a novel azetidinyl ketolide antibiotic is described. Starting with clarithromycin, the eight-step…”
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Process Development of CP-481715, a Novel CCR1 Antagonist by Li, Bryan, Andresen, Brian, Brown, Matthew F, Buzon, Richard A, Chiu, Charles K.-F, Couturier, Michel, Dias, Eric, Urban, Frank J, Jasys, V. John, Kath, John C, Kissel, William, Le, Tung, Li, Z. Jane, Negri, Joanna, Poss, Christopher S, Tucker, John, Whritenour, David, Zandi, Kathleen

“…Process development for the synthesis of 2-quinoxalinecarboxamide, N-[(1S,2S,4R)-4-(aminocarbonyl)-1-[(3-fluorophenyl)methyl]-2,7-dihydroxy-7-methyloctyl] is…”
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Case Study of a γ-Butyrolactone Alkylation with 1,3-Dimethyl-2-imidazolidinone as a Promoter by Li, Bryan, Buzon, Richard A, Castaldi, Michael J

“…1,3-Dimethyl 2-imidazolidinone (DMI) is of lower toxicological risk than 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone (DMPU), hexamethyl-phosphorus…”
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Utilization of ReactIR in Fit for Purpose Process Enablement by Eisenbeis, Shane A, Chen, Raymond, Kang, Ming, Barrila, Mark, Buzon, Richard

“…An efficient four-step synthesis of 1 is described in which utilization of ReactIR was key to efficient processing and reaction monitoring. Key chemical steps…”
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Novel tethers in ketolide antibiotics by Kaneko, Takushi, Romero, Karina, Li, Bryan, Buzon, Richard

“…Novel tethers for ketolide analogues were developed using the Curtius rearrangement. The resulting compounds show potent in vitro and in vivo activity. Novel…”
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Process Research and Large-Scale Synthesis of 4‘‘,6‘‘-Bis((2-fluorophenyl)carbamoyl)hecogenyl β-O-Cellobioside:  A Potent Cholesterol Absorption Inhibitor by Urban, Frank J, Breitenbach, Ralph, Buzon, Richard A, Daniels, Peter J, Dunn, Peter J, Gut, Sally, Lehner, Richard S, Orrill, Susan L, Watson, Harry A

“…This paper describes process research leading to the successful scale-up of a potent cholesterol absorption inhibitor…”
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Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections by Magee, Thomas V, Ripp, Sharon L, Li, Bryan, Buzon, Richard A, Chupak, Lou, Dougherty, Thomas J, Finegan, Steven M, Girard, Dennis, Hagen, Anne E, Falcone, Michael J, Farley, Kathleen A, Granskog, Karl, Hardink, Joel R, Huband, Michael D, Kamicker, Barbara J, Kaneko, Takushi, Knickerbocker, Michael J, Liras, Jennifer L, Marra, Andrea, Medina, Ivy, Nguyen, Thuy-Trinh, Noe, Mark C, Obach, R. Scott, O’Donnell, John P, Penzien, Joseph B, Reilly, Usa Datta, Schafer, John R, Shen, Yue, Stone, Gregory G, Strelevitz, Timothy J, Sun, Jianmin, Tait-Kamradt, Amelia, Vaz, Alfin D. N, Whipple, David A, Widlicka, Daniel W, Wishka, Donn G, Wolkowski, Joanna P, Flanagan, Mark E

“…Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1)…”
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Aqueous phosphoric acid as a mild reagent for deprotection of the t-butoxycarbonyl group by Li, Bryan, Bemish, Raymond, Buzon, Richard A., Chiu, Charles K.-F., Colgan, Stephen T., Kissel, William, Le, Tung, Leeman, Kyle R., Newell, Lisa, Roth, Joshua

“…Aqueous phosphoric acid (85 wt%) is an efficient and mild reagent for the deprotection of N-BOC groups. Acid sensitive functionalities including benzyl and…”
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Stereoselective synthesis of 5-[(1 S)- N-Boc-amino-(2 S)-(3-fluorophenyl)ethyl]-dihydrofuran-2-one by Li, Bryan, Buzon, Richard A., Chiu, Charles K.-F., Colgan, Stephen T., Jorgensen, Matthew L., Kasthurikrishnan, Narasim

“…Phthalic anhydride as thiolate scavenger effectively preserved the enantiopurity of α-aminoketone, thus affording the convenient synthesis of the titled…”
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Novel Synthesis of 1-(1,2,3,5,6,7-Hexahydro- s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl]urea, an Anti-inflammatory Agent by Urban, Frank J., John Jasys, V., Raggon, Jeffrey W., Buzon, Richard A., Hill, Paul D., Eggler, James F., Weaver, John D.

“…A novel synthesis of the anti-inflammatory agent 1-(1,2,3,5,6,7- hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl] urea 1 is…”
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