219499-19-1Relevant academic research and scientific papers
Oxidative fluorination of N-arylsulfonamides
Buckingham, Faye,Calderwood, Samuel,Checa, Bego?a,Keller, Thomas,Tredwell, Matthew,Collier, Thomas Lee,Newington, Ian M.,Bhalla, Rajiv,Glaser, Matthias,Gouverneur, Véronique
, p. 33 - 39 (2015/09/22)
We report a late stage oxidative nucleophilic fluorination of N-arylsulfonamides, a class of compounds so far not considered as precursors to 4-fluorophenyl sulfonamides. By installing a para-positioned tert-butyl substituent on the aniline, oxidative fluorination takes place regioselectively in the presence of HF·pyridine and PIDA. This methodology has been shown to give good yields for a variety of ortho- and meta-functionalised N-arylsulfonamides and has been adapted for radiofluorination to give 4-[18F]fluorophenyl sulfonamides under carrier added conditions.
Acylative Suzuki coupling of amides: Acyl-nitrogen activation via synergy of independently modifiable activating groups
Li, Xijing,Zou, Gang
supporting information, p. 5089 - 5092 (2015/03/30)
A highly efficient palladium-catalyzed acylative cross-coupling of carboxylic amides with arylboronic acids has been achieved via synergistic activation of the Cacyl-N bond by independently modifiable activating groups. Coupling of amides features not only good functional group tolerance but also modifiable reactivities to overcome steric hindrance. This journal is
Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists
Torisu, Kazuhiko,Kobayashi, Kaoru,Iwahashi, Maki,Nakai, Yoshihiko,Onoda, Takahiro,Nagase, Toshihiko,Sugimoto, Isamu,Okada, Yutaka,Matsumoto, Ryoji,Nanbu, Fumio,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
, p. 5361 - 5378 (2007/10/03)
N-(p-Alkoxy)benzoyl-2-methylindole-4-acetic acids 2r and 2s were identified as a new class of orally active prostaglandin D2 (PGD2) receptor antagonists. The process of discovering a series of N-(p-alkoxy)benzoyl-2-methylindole-4-ace
Discovery of orally active prostaglandin D2 receptor antagonists
Torisu, Kazuhiko,Kobayashi, Kaoru,Iwahashi, Maki,Nakai, Yoshihiko,Onoda, Takahiro,Nagase, Toshihiko,Sugimoto, Isamu,Okada, Yutaka,Matsumoto, Ryoji,Nanbu, Fumio,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
, p. 4891 - 4895 (2007/10/03)
Discovery process of a new PGD2 receptor antagonists 3i is reported. A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D2 (DP) receptor affinity and antagonist activity. So
