2968-13-0Relevant articles and documents
Synthesis of α-arylthioacetones using TEMPO as the: C 3 synthon via a reaction cascade of sequential oxidation, skeletal rearrangement and C-S bond formation
Zou, Jiao-Xia,Jiang, Yi,Lei, Shuai,Yin, Gao-Feng,Hu, Xiao-Ling,Zhao, Quan-Yi,Wang, Zhen
supporting information, p. 2341 - 2345 (2019/03/07)
Here, we present an unprecedented pathway to α-sulfenylated carbonyl compounds from commercially available thiols and universally employed TEMPO and its analogues, which act as C3 synthons through skeletal rearrangement under simple and metal-f
Total Synthesis of the Reported Structure of Stresgenin B Enabled by the Diastereoselective Cyanation of an Oxocarbenium
Chan, Wei Chuen,Koide, Kazunori
supporting information, p. 7798 - 7802 (2019/01/04)
We report the first total synthesis of the reported structure of the heat shock protein expression inhibitor stresgenin B. The synthesis features (1) diastereoselective cyanation of an oxocarbenium intermediate en route to the synthetically challenging α-
A sulfur-containing amino acid amide carbamate derivative and application thereof
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Paragraph 0033-0034; 0038-0039, (2017/08/09)
The invention belongs to the field of plant fungicides, and relates to sulfur-containing amino acid amide carbamate derivatives of which the general formulas I are shown in the description and pharmaceutically acceptable salts of the sulfur-containing amino acid amide carbamate derivatives. In the general formulas I, substituent groups R1, R2 and n are defined in the description. The invention further relates to preparation methods of compounds related to the general formulas I, special intermediates developed for the preparation of the compounds, and application of the compounds to prevention and control of plant diseases.
α-Arylchalcogenation of acetone with diaryl dichalcogenide via metal-free oxidative C(sp3)-H bond functionalization
Yan, Guobing,Borah, Arun Jyoti,Wang, Lianggui,Pan, Zhangjin,Chen, Shuangshuang,Shen, Xuqian,Wu, Xiangmei
, p. 4305 - 4307 (2015/06/22)
Direct α-arylchalcogenation of acetone with diaryl dichalcogenides has been achieved by using a mixture of TBHP and DTBP oxidants at 120 °C without transition-metal catalyst via oxidative C(sp3)-H bond functionalization. The method exhibits good functional group tolerance and products were isolated in moderate to high yields.
Electrophilic substitution reactions using an electrogenerated ArS(ArSSAr)+ cation pool as an ArS+ equivalent
Matsumoto, Kouichi,Kozuki, Yuki,Ashikari, Yosuke,Suga, Seiji,Kashimura, Shigenori,Yoshida, Jun-Ichi
, p. 1916 - 1919 (2012/05/05)
Arylbis(arylthio)sulfonium ions (ArS(ArSSAr)+), which were generated and accumulated by the low-temperature electrolysis of diaryl disulfide (ArSSAr), were found to serve as ArS+ equivalent in electrophilic substitution reactions of
Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands
Mésangeau, Christophe,Fraise, Mika?l,Delagrange, Philippe,Caignard, Daniel Henri,Boutin, Jean Albert,Berthelot, Pascal,Yous, Sa?d
experimental part, p. 1835 - 1840 (2011/05/06)
A series of N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)acylamides was synthesized and evaluated for binding affinity and intrinsic activity at melatonin receptors. The affinity of each compound for the melatonin receptors was determined by binding studies on cloned human MT 1 and MT2 receptors expressed in CHO cells. Agonist and antagonist potency was measured on the [35S]GTPγS binding assay for the most interesting compounds. The new derivatives 8-14 showed modest to high selectivity (between 4 and 220) for MT2 receptors. The most selective compound, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)but-3-enamide (14), an MT2 ligand with affinity for the MT 2 receptor similar to that of melatonin and a 220-fold preference over MT1 receptors, acts as a partial agonist. In addition, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl)ethyl)propionamide (9), a nanomolar MT2 ligand with a good selectivity ratio (MT 1/MT2 = 51) shows antagonist activity on both melatonin receptors.
HETEROCYCLIC DIHYDROPYRIMIDINE COMPOUNDS
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Page/Page column 45-46, (2008/06/13)
Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra rapidly activating d
Synthesis, anti-mycobacterial, anti-trichomonas and anti-candida in vitro activities of 2-substituted-6,7-difluoro-3-methylquinoxaline 1,4-dioxides
Carta, Antonio,Loriga, Mario,Paglietti, Giuseppe,Mattana, Antonella,Fiori, Pier Luigi,Mollicotti, Paola,Sechi, Leonardo,Zanetti, Stefania
, p. 195 - 203 (2007/10/03)
A new series of 23 6,7-difluoro-3-methyl-2-phenylthio/phenylsulfonyl/ phenylsulfinyl/benzylamino/phenylamino-quinoxaline 1,4-dioxides variously substituted in the phenyl moiety, was synthesized and submitted to in vitro evaluation for anti-mycobacterial,
C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.
Matsunaga, Nobuyuki,Kaku, Tomohiro,Itoh, Fumio,Tanaka, Toshimasa,Hara, Takahito,Miki, Hiroshi,Iwasaki, Masahiko,Aono, Tetsuya,Yamaoka, Masuo,Kusaka, Masami,Tasaka, Akihiro
, p. 2251 - 2273 (2007/10/03)
Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h, (S)-9i, and 9k with nanomolar enzyme inhibition (IC(50)=4-9 nM) and 9e (IC(50)=27 nM) were identified to have powerful in vivo efficacy with extended duration of action. The key structural determinants for the in vivo efficacy were demonstrated to be the 5-fluoro group on the benzothiophene ring and the 4-imidazolyl moiety. Superimposition of 9k and 17 alpha-hydroxypregnenolone demonstrated their structural similarity and enabled rationalization of the pharmacological results. In addition, selected compounds were also identified to be potent inhibitors of human enzyme with IC(50) values of 20-30 nM.
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors
Masaki, Hidekazu,Mizuno, Yusuke,Tatui, Akira,Murakami, Akira,Koide, Yuuki,Satoh, Shoji,Takahashi, Atsuo
, p. 4085 - 4088 (2007/10/03)
We have identified a new class of chymase inhibitor through a substituent analysis of MWP00965, which we previously discovered by in silico screening. TY-51076 (7) showed high potency (IC50=56 nM) and excellent selectivity for chymase compared to chymotrypsin and cathepsin G (>400-fold). The synthesis and structure-activity relationship of this class are described.