53976-65-1Relevant articles and documents
Nature of the Nucleophilic Oxygenation Reagent Is Key to Acid-Free Gold-Catalyzed Conversion of Terminal and Internal Alkynes to 1,2-Dicarbonyls
Dubovtsev, Alexey Yu.,Shcherbakov, Nikolay V.,Dar'in, Dmitry V.,Kukushkin, Vadim Yu.
, p. 745 - 757 (2020/02/04)
2,3-Dichloropyridine N-oxide, a novel oxygen transfer reagent, allows the conductance of the gold(I)-catalyzed oxidation of alkynes to 1,2-dicarbonyls in the absence of any acid additives and under mild conditions to furnish the target species, including those derivatized by highly acid-sensitive groups. The developed strategy is effective for a wide range of alkyne substrates such as terminal- and internal alkynes, ynamides, alkynyl ethers/thioethers, and even unsubstituted acetylene (40 examples; yields up to 99%). The oxidation was successfully integrated into the trapping of reactive dicarbonyls by one-pot heterocyclization and into the synthesis of six-membered azaheterocycles. This synthetic acid-free route was also successfully applied for the total synthesis of a natural 1,2-diketone.
Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor
Ando, Makoto,Sato, Nagaaki,Nagase, Tsuyoshi,Nagai, Keita,Ishikawa, Shiho,Takahashi, Hirobumi,Ohtake, Norikazu,Ito, Junko,Hirayama, Mioko,Mitobe, Yuko,Iwaasa, Hisashi,Gomori, Akira,Matsushita, Hiroko,Tadano, Kiyoshi,Fujino, Naoko,Tanaka, Sachiko,Ohe, Tomoyuki,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro
experimental part, p. 6106 - 6122 (2009/12/24)
A series of 2-pyridone-containing imidazoline derivatives was synthesized and evaluated as neuropeptide Y Y5 receptor antagonists. Optimization of the 2-pyridone structure on the 2-position of the imidazoline ring led to identification of 1-(difluoromethy