Zobrazeno 1 - 10 of 24 pro vyhledávání: '"Seble Wagaw"'
1
Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor
Autor: Seble Wagaw, Andrew S. Judd, Jianzhang Mei, Kenneth M. Engstrom, Andrew J. Souers, Gang Zhao, Brian J. Kotecki, Philip R. Kym, Matthew M. Ravn
Publikováno v: Organic Process Research & Development. 14:417-424
A synthesis of a selective diacyl glycerolacyltransferase-1 (DGAT-1) inhibitor, 1, is described. The synthesis illustrates a diketone Favorskii reaction on 9 in place of the more common ketoester variant for generation of the dicarboxycyclopentane co
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dde9159c7cd78e997230e4074fbe58d4
https://doi.org/10.1021/op900310v
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2
Development of a Scalable Synthesis of Dipeptidyl Peptidase-4 Inhibitor ABT-279
Autor: Michael J. Rozema, Albert W. Kruger, Lakshmi Bhagavatula, Kenneth M. Engstrom, Thomas B. Borchardt, Jorge Gandarilla, Todd S. McDermott, Brian J. Kotecki, Ahmad Y. Sheikh, Steven J. Wittenberger, Seble Wagaw
Publikováno v: Organic Process Research & Development. 13:1145-1155
A convergent, scalable synthesis of dipeptidyl peptidase-4 inhibitor, ABT-279, has been developed and demonstrated on multikilogram scale. The cis-2,5-disubstituted pyrrolidine is generated by cyclization of a Boc-amine onto an alkynyl ketone followe
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ee9b10f3b45e07e63d7f7527687b1fbe
https://doi.org/10.1021/op900197r
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3
A Convergent Process for the Preparation of Adamantane 11-β-HSD-1 Inhibitors
Autor: John C. Tolle, Francis A. J. Kerdesky, Seble Wagaw, Calvin L. Becker, Weifeng Wang, Kenneth M. Engstrom
Publikováno v: Organic Process Research & Development. 12:1114-1118
A convergent, scalable process was developed for the synthesis of adamantane 11-β-hydroxysteroid dehydrogenase-1 inhibitors E-4-(2-methyl-2-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)propionylamino)adamantane-1-carboxylic acid (1) and E-4-(2
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::df6ec9b256cacaf931d62b26c5260219
https://doi.org/10.1021/op800065q
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4
An Efficient, Stereoselective Synthesis of the Hydroxyethylene Dipeptide Isostere Core for the HIV Protease Inhibitor A-792611
Autor: Rodger F. Henry, Yu-Ming Pu, Weifeng Wang, L. Steven Hollis, Ian Marsden, Brian J. Kotecki, Seble Wagaw, Kenneth M. Engstrom
Publikováno v: The Journal of Organic Chemistry. 71:5369-5372
A stereoselective synthesis of the hydroxyethylene dipeptide isostere 1 is described. The route employs a substrate-directed kinetic protonation of an alpha/gamma-substituted lactone to afford the desired stereochemistry. A method for converting the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0760496819e9a76c5e14dbd8a54ded33
https://doi.org/10.1021/jo060737s
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6
Development of a Catalytic Enantioselective Conjugate Addition of 1,3-Dicarbonyl Compounds to Nitroalkenes for the Synthesis of Endothelin-A Antagonist ABT-546. Scope, Mechanism, and Further Application to the Synthesis of the Antidepressant Rolipram
Autor: Seble Wagaw, Jianguo Ji, Michael A Fitzgerald, Michael G. Fickes, David M. Barnes, Frederick A. Plagge, Margo Preskill, Steven A. King, Steven J. Wittenberger, Ji Zhang, Howard E. Morton
Publikováno v: Journal of the American Chemical Society. 124:13097-13105
The enantioselective synthesis of endothelin-A antagonist ABT-546 has been accomplished via the discovery and development of a highly selective catalytic asymmetric conjugate addition of ketoesters to nitroolefins. Employing just 4 mol % bis(oxazolin
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9fd40e87e9cded6c7ab9ee255e355fa
https://doi.org/10.1021/ja026788y
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7
A Palladium-Catalyzed Method for the Preparation of Indoles via the Fischer Indole Synthesis
Autor: Stephen L. Buchwald, Seble Wagaw, and Bryant H. Yang
Publikováno v: Journal of the American Chemical Society. 121:10251-10263
A Pd-catalyzed method for the preparation of N-aryl benzophenone hydrazones 4 is described. The use of a Pd/BINAP-based catalyst provides hydrazones 4 in good yields. Using 0.1 mol % of a Pd/9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (Xantphos)
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::63ce393915665085a499eb6e113c7cb5
https://doi.org/10.1021/ja992077x
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9
Palladium-Catalyzed Coupling of Optically Active Amines with Aryl Bromides
Autor: Seble Wagaw, Stephen L. Buchwald, and Roger A. Rennels
Publikováno v: Journal of the American Chemical Society. 119:8451-8458
The coupling of enantiomerically enriched amines with aryl bromides produces the corresponding N-aryl derivatives. The choice of ligand in the palladium-catalyzed coupling is critical to the format...
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fbb1a9c63b9b357aee3e08d17b0dfe73
https://doi.org/10.1021/ja971583o
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