74672-02-9Relevant academic research and scientific papers
ANTIBIOTIC COMPOUNDS
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Page/Page column 78; 79, (2018/03/25)
The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
An efficient, direct bis-ortho-chlorination of 4-(difluoromethoxy)aniline and its application to the synthesis of BMS-665053, a potent and selective pyrazinone-containing corticotropin-releasing factor-1 receptor antagonist
Li, Jianqing,Smith, Daniel,Krishnananthan, Subramaniam,Hartz, Richard A.,Dasgupta, Bireshwar,Ahuja, Vijay,Schmitz, William D.,Bronson, Joanne J.,Mathur, Arvind,Barrish, Joel C.,Chen, Bang-Chi
scheme or table, p. 156 - 159 (2012/05/20)
An efficient scale-up synthesis of (S)-5-chloro-1-(1-cyclopropylethyl)-3- (2,6-dichloro-4-(difluoromethoxy)phenylamino)-pyrazin-2(1H)-one, 1 (BMS-665053), is described. This new process features a one-step direct bis-ortho- chlorination of 4-(difluorometh
Synthesis of sterically hindered polychlorinated biphenyl derivatives
Joshi,Vyas,Duffel,Parkin,Lehmler
experimental part, p. 1045 - 1054 (2011/06/20)
A series of sterically hindered (methoxylated) polychlorinated biphenyl derivatives were synthesized using the Suzuki and the Ullmann coupling reactions. The Suzuki coupling with Pd(dba)2-dicyclohexylphosphino-2,6- dimethoxybiphenyl (DPDB) gave better yields (65-98%) compared to the classic Ullmann coupling reaction (20-38%). Despite the reactive catalyst system, no significant coupling with aromatic chlorine substituents was observed. Crystal structure analysis of four PCB derivatives revealed solid state dihedral angles ranging from 69.7 to 81.0, which indicates that these highly ortho-substituted PCB derivatives have some conformational flexibility. Georg Thieme Verlag Stuttgart.
In vitro intrinsic clearance-based optimization of N3- phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz, Richard A.,Ahuja, Vijay T.,Rafalski, Maria,Schmitz, William D.,Brenner, Allison B.,Denhart, Derek J.,Ditta, Jonathan L.,Deskus, Jeffrey A.,Yue, Eddy W.,Arvanitis, Argyrios G.,Lelas, Snjezana,Li, Yu-Wen,Molski, Thaddeus F.,Wong, Harvey,Grace, James E.,Lentz, Kimberley A.,Li, Jianqing,Lodge, Nicholas J.,Zaczek, Robert,Combs, Andrew P.,Olson, Richard E.,Mattson, Ronald J.,Bronson, Joanne J.,Macor, John E.
experimental part, p. 4161 - 4172 (2010/02/28)
A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropinreleasing factor-1 (CRF1) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic proper
Synthesis of deuterium labelled 4'-hydroxydiclofenac
Waterhouse, Ian
, p. 1075 - 1083 (2007/10/03)
Diclofenac is a potentially useful substrate for the study of drug-drug interactions caused by modulation of the activity of specific isoforms of cytochrome P450. The synthesis of a deuterium labelled version of its principal human metabolite, 4'-hydroxydiclofenac, for use as an internal standard in LC-MS-MS studies, is described.
