Zobrazeno 1 - 10
of 19
pro vyhledávání: '"David J. Fairfax"'
Autor:
Janet Dell-John, John D. Dimarco, Cheryl A. Rizzo, Mark E. Salvati, Steven H. Spergel, Gregory Scott Martin, Weifang Shan, Aaron Balog, Georgia Cornelius, Richard Rampulla, Marco M. Gottardis, Andrew Nation, Christian L. Holst, Liang Schweizer, Gregory D. Vite, Lana M. Rossiter, Ricardo M. Attar, David J. Fairfax, Thomas E. Spires, Stanley R. Krystek, George L. Trainor, Jack Z. Gougoutas
Publikováno v:
ACS Medicinal Chemistry Letters. 6:908-912
BMS-641988 (23) is a novel, nonsteroidal androgen receptor antagonist designed for the treatment of prostate cancer. The compound has high binding affinity for the AR and acts as a functional antagonist in vitro. BMS-641988 is efficacious in multiple
Autor:
Timothy Rust, Carla Hassler, James P. Harding, Justin J. Richards, Brian I. Bliss, Yuri L. Khmelnitsky, David D. Manning, Marlene L. Cohen, Liaqat Masih, Michael A. Lynch, Jianqing Chen, Kevin L. Christensen, Zhicai Yang, Soshanna Isaacson, Jonathan D. Wierschke, Cathy M. Beer, Russell J. DeOrazio, Jun-Ho Maeng, Lisa H. Peterson, Christopher L. Cioffi, Alexander Usyatinsky, Kevin Fitzpatrick, David J. Fairfax, Matthew Isherwood, Svetlana Dobritsa, W. Martin Rennells
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6538-6541
A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT(3) receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT(3)A receptors. A chemistry optimization program was co
Autor:
Hai-Yun Xiao, Jieping Geng, David J. Fairfax, Thomas E. Spires, Wen-Ching Han, Marco M. Gottardis, Mark E. Salvati, Andrew Nation, Weifang Shan, Mary-Ellen Cvjic, Jing Chen, Liang Schweizer, Mary T. Obermeier, Gregory Scott Martin, Ricardo M. Attar, Gregory D. Vite, Aaron Balog, Ashvinikumar V. Gavai, Janet Dell-John, Cheryl A. Rizzo, Lana M. Rossiter, Linda B. Fleming, Christian L. Holst
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4491-4495
A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were fou
Autor:
Robert Lewis, David J. Fairfax, David M. Jenkins, Andrew J. Zych, Hong-Jun Wang, Rajiv R. Srivastava, William G. Earley
Publikováno v:
Tetrahedron Letters. 48:3043-3046
A highly efficient one-pot, two-step microwave procedure has been developed for the synthesis of 4-substituted 1-heteroarylpiperazines. Microwave heating of heteroaryl chlorides with 1,4-diazabicyclo[2.2.2]octane (DABCO) at 160 °C for 15 min yielded
Autor:
David J. Fairfax, Rajiv R. Srivastava, Hong-Jun Wang, David M. Jenkins, Andrew J. Zych, Zhen‐Jia Chen
Publikováno v:
Synthetic Communications. 37:431-438
A variety of aryl nitriles were prepared in excellent yield from the palladium(II) acetate–catalyzed cross‐coupling of aryl triflates and zinc cyanide under microwave irradiation conditions. To facilitate purification, polymer‐supported triphen
Publikováno v:
Synlett. 2006:0379-0382
A one-pot method for the preparation of 1,8-naphthyridine derivatives is reported. The method involves the dimetalation of an appropriate N-2-pyridylpivalamide or tert-butylcarbamate followed by reaction with a β-dimethylamino or β-alkoxyacrolein d
Preparation of 5-(2-Methoxy-4-nitrophenyl)oxazole: A Key Intermediate for the Construction of VX-497
Publikováno v:
Organic Process Research & Development. 6:677-681
A process for the multigram preparation of 5-(2-methoxy-4-nitrophenyl)oxazole, a key intermediate for the preparation of the hepatitis C drug candidate VX-497 (merimepodib), has been achieved in good yield from a commercially available dye. Early stu
Autor:
Gregory Scott Martin, David J. Fairfax, Lisa H. Bourdon, Casey J. N. Mathison, Pavel Zhichkin
Publikováno v:
Tetrahedron: Asymmetry. 15:3485-3487
A method for the preparation of (2R,3S) nitrogen protected arylserine esters is described. The method consists of rhodium mediated insertion of tert-butylcarbamate into the corresponding 3-keto-2-diazoester, affording the N-protected α-amino-β-keto
Publikováno v:
Synthesis. 2002:720-722
A method for the synthesis of 2-substituted pyrimidine-5-carboxylic esters is described. The sodium salt of 3,3-dimethoxy-2-methoxycarbonylpropen-1-ol (3) has been found to react with a variety of amidinium salts to afford the corresponding 2-substit
Autor:
Albert Padwa, David J. Fairfax, Ugo Chiacchio, S. L. Xu, Mark A. Semones, Jamal M. Kassir, Angelo Litrico
Publikováno v:
The Journal of Organic Chemistry. 58:6429-6437
The photochemical, thermal, and rhodium-catalyzed decomposition reactions of several closely related o-alkynyl or o-alkenyl α-diazoaceto- and propiophenone derivatives have been studied. The reaction outcome is markedly dependent upon the reaction c