33209-75-5Relevant articles and documents
A heavy-metal-free desulfonylative Giese-type reaction of benzothiazole sulfones under visible-light conditions
Inuzuka, Toshiyasu,Iwama, Haruka,Ogawa, Daichi,Sengoku, Tetsuya,Yoda, Hidemi
, p. 9858 - 9861 (2021/10/12)
A visible-light-induced desulfonylative Giese-type reaction has been developed. Essential to the success is the employment of Hantzsch ester to activate benzothiazole sulfones without any heavy-metal additives. Not only benzylic benzothiazole sulfones but also alkyl ones were viable substrates and reacted with electron-deficient alkenes and a propiol amide.
Design, synthesis, and evaluation of novel inhibitors for wild-type human serine racemase
Takahara, Satoyuki,Nakagawa, Kiyomi,Uchiyama, Tsugumi,Yoshida, Tomoyuki,Matsumoto, Kazunori,Kawasumi, Yasuo,Mizuguchi, Mineyuki,Obita, Takayuki,Watanabe, Yurie,Hayakawa, Daichi,Gouda, Hiroaki,Mori, Hisashi,Toyooka, Naoki
supporting information, p. 441 - 445 (2017/12/28)
Most of the endogenous free D-serine (about 90%) in the brain is produced by serine racemase (SR). D-Serine in the brain is involved in neurodegenerative disorders and epileptic states as an endogenous co-agonist of the NMDA-type glutamate receptor. Thus, SR inhibitors are expected to be novel therapeutic candidates for the treatment of these disorders. In this study, we solved the crystal structure of wild-type SR, and tried to identify a new inhibitor of SR by in silico screening using the structural information. As a result, we identified two hit compounds by their in vitro evaluations using wild-type SR. Based on the structure of the more potent hit compound 1, we synthesized 15 derivatives and evaluated their inhibitory activities against wild-type SR. Among them, the compound 9C showed relatively high inhibitory potency for wild-type SR. Compound 9C was a more potent inhibitor than compound 24, which was synthesized by our group based upon the structural information of the mutant-type SR.
STUDIES ON OXYGEN HETEROCYCLES PART-1 : ACID CATALYSED AND PHOTOCHEMICAL REACTIONS OF SOME ARYLDIAZOKETONES
Ghosh, Somnath,Datta, Indira,Chakraborty, Rupak,Das, Tapas Kumar,Sengupta, Judhajit,Sarkar, Dipak Chandra
, p. 1441 - 1446 (2007/10/02)
Trifluoroacetic acid catalysed reaction of 2-methoxyphenyldiazomethylketone (4a), 2-acetoxyphenyldiazomethylketone (4b) and 3-(2-anisyl)-α-diazo-2-propanone (11) leads to the formation of coumaranone (6) and 3-chromanone (12), while 4-(2-anisyl)-α-diazo-2-butanone (16) affords benzo-1-oxepan-3-one (17) and 5-methoxy-2-tetralone (18) in moderate yield.The photochemical decomposition of the said diazoketones (4a, 11 and 16) gave products depending on the length of the side chain present in the substrates.