763902-92-7Relevant academic research and scientific papers
4-[5-Fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]phenyl]-3,4,5, 6-tetrahydro-2H-pyran-4-carboxamide, an Orally Active Inhibitor of 5-Lipoxygenase with Improved Pharmacokinetic and Toxicology Characteristics
Mano, Takashi,Okumura, Yoshiyuki,Sakakibara, Minoru,Okumura, Takako,Tamura, Tetsuya,Miyamoto, Kimitaka,Stevens, Rodney W.
, p. 720 - 725 (2004)
Described herein are structure- activity relationships (SARs) of 4-[5-fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]-phenyl]-4-methoxy-3,4,5, 6-tetrahydro-2H-pyran (1, CJ-12,918), an imidazole 5-lipoxygenase (5-LO) inhibitor. When 1 was tested in precl
Efficient synthesis of 4-(3-fluoro-5-{[4-(2-methyl-1h-imidazol-1-yl)benzyl] -oxy}phenyl)tetrahydro-2h-pyran-4-carboxamide, a novel 5-lipoxygenase inhibitor
Mano, Takashi,Stevens, Rodney W.,Nakao, Kazunari,Okumura, Yoshiyuki,Kawamura, Kiyoshi,Ando, Akemi,Matsuoka, Yoko
, p. 2625 - 2628 (2007/10/03)
An efficient synthesis of 1, a novel orally active 5-lipoxygenase inhibitor, was developed. Key features of the modified synthetic route include facile construction of the benzyl phenyl ether moiety by nucleophilic aromatic substitution and THP ring by cyclization, and base-promoted hydrolysis of the nitrile group to carboxamide. The improved three-step synthesis provides 25 g of 1 for pre-clinical toxicology studies in a total yield of 59%.
2-substituted-1(4)-aryl piperazines and the process for their preparation
-
, (2008/06/13)
This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects and are of the following general formula I
