- 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
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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
- Zou, Jiao-Xia,Jiang, Yi,Lei, Shuai,Yin, Gao-Feng,Hu, Xiao-Ling,Zhao, Quan-Yi,Wang, Zhen
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supporting information
p. 2341 - 2345
(2019/03/07)
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- Total Synthesis of the Reported Structure of Stresgenin B Enabled by the Diastereoselective Cyanation of an Oxocarbenium
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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-
- Chan, Wei Chuen,Koide, Kazunori
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supporting information
p. 7798 - 7802
(2019/01/04)
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- A sulfur-containing amino acid amide carbamate derivative and application thereof
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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.
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Paragraph 0033-0034; 0038-0039
(2017/08/09)
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- α-Arylchalcogenation of acetone with diaryl dichalcogenide via metal-free oxidative C(sp3)-H bond functionalization
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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.
- Yan, Guobing,Borah, Arun Jyoti,Wang, Lianggui,Pan, Zhangjin,Chen, Shuangshuang,Shen, Xuqian,Wu, Xiangmei
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supporting information
p. 4305 - 4307
(2015/06/22)
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- Electrophilic substitution reactions using an electrogenerated ArS(ArSSAr)+ cation pool as an ArS+ equivalent
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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
- Matsumoto, Kouichi,Kozuki, Yuki,Ashikari, Yosuke,Suga, Seiji,Kashimura, Shigenori,Yoshida, Jun-Ichi
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p. 1916 - 1919
(2012/05/05)
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- Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands
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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.
- Mésangeau, Christophe,Fraise, Mika?l,Delagrange, Philippe,Caignard, Daniel Henri,Boutin, Jean Albert,Berthelot, Pascal,Yous, Sa?d
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experimental part
p. 1835 - 1840
(2011/05/06)
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- HETEROCYCLIC DIHYDROPYRIMIDINE COMPOUNDS
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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
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Page/Page column 45-46
(2008/06/13)
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- Synthesis, anti-mycobacterial, anti-trichomonas and anti-candida in vitro activities of 2-substituted-6,7-difluoro-3-methylquinoxaline 1,4-dioxides
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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,
- Carta, Antonio,Loriga, Mario,Paglietti, Giuseppe,Mattana, Antonella,Fiori, Pier Luigi,Mollicotti, Paola,Sechi, Leonardo,Zanetti, Stefania
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p. 195 - 203
(2007/10/03)
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- C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.
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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.
- Matsunaga, Nobuyuki,Kaku, Tomohiro,Itoh, Fumio,Tanaka, Toshimasa,Hara, Takahito,Miki, Hiroshi,Iwasaki, Masahiko,Aono, Tetsuya,Yamaoka, Masuo,Kusaka, Masami,Tasaka, Akihiro
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p. 2251 - 2273
(2007/10/03)
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- Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors
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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.
- Masaki, Hidekazu,Mizuno, Yusuke,Tatui, Akira,Murakami, Akira,Koide, Yuuki,Satoh, Shoji,Takahashi, Atsuo
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p. 4085 - 4088
(2007/10/03)
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- α-alkyl-α-amino-β-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1
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A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected comp
- Becker, Daniel P,DeCrescenzo, Gary,Freskos, John,Getman, Daniel P,Hockerman, Susan L,Li, Madeleine,Mehta, Pramod,Munie, Grace E,Swearingen, Craig
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p. 2723 - 2725
(2007/10/03)
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- Optionally substituted phenylimidazolidines, their preparation process and intermediates, their use as medicaments and the pharmaceutical compositions containing them
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A compound in all possible racemic, enantiomeric and diastereoisomer forms of the formula STR1 wherein Y is --O--, Z 2 is --CF 3, Z 1 is --CN or --NO 2, X is --O-- or --S--, R 3 is hydrogen or alkyl of 1 to 4 carbon atoms optionally substituted by at least one halogen or --CN and R 4 and R 5 are individually alkyl of 1 to 4 carbon atoms optionally substituted with a member of the group consisting of halogen, --OH, esterified or etherified or protected hydroxy and phenylthio optionally substituted by halogen or --OH, and wherein at least one of R 4 and R 5 is substituted having antiandrogenic activity.
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