1442-03-1Relevant articles and documents
Facile syntheses of 3-trifluoromethylthio substituted thioflavones and benzothiophenes via the radical cyclization
Wang, Lu,Wang, Huaiyu,Meng, Weidong,Xu, Xiu-Hua,Huang, Yangen
supporting information, p. 389 - 392 (2020/03/04)
3-CF3S substituted thioflavones and benzothiophenes were achieved via the reactions of AgSCF3 with methylthiolated alkynones and alkynylthioanisoles, respectively, promoted by persulfate. This protocol possesses good functional group tolerance and high yields. Mechanistic studies suggested that a classic two-step radical process was involved, which includes addition of CF3S radical to triple bond and cyclization with SMe moiety.
Synthetic method 1-2 - benzisothiazol -3 -one compound (by machine translation)
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Paragraph 0022-0024; 0032-0034; 0035-0037, (2020/09/09)
The invention discloses a synthetic method of 1-2 - benzisothiazol -3 -one compound, and belongs to the field of chemical synthesis. 2 - 1-benzisothiazol 2 -one compounds are synthesized through acid chlorination, amidation and cyclization reaction by using the sulfenyl-substituted benzoic acid extracted from BIT process -3 - waste water as a starting raw material. The method disclosed by the invention has the advantages of mild reaction conditions, simple and convenient operation, strong practicability, less waste water, high product purity and the like, and is suitable for large-scale industrial production. The technical scheme provided by the invention is resource utilization and preparation 1 of wastewater extract produced in BIT production, and a feasible method is provided for the 2 -benzisothiazol -3 -one compound. (by machine translation)
Mapping the Interactions of I2, I., I-, and I+ with Alkynes and Their Roles in Iodocyclizations
Volpe, Rohan,Aurelio, Luigi,Gillin, Murray G.,Krenske, Elizabeth H.,Flynn, Bernard L.
supporting information, p. 10191 - 10199 (2015/07/07)
A combination of experiment and theory has been used to explore the mechanisms by which molecular iodine (I2) and iodonium ions (I+) activate alkynes towards iodocyclization. Also included in the analysis are the roles of atomic iodi
Synthesis, spectral characterization and electrochemical properties of (2-alkylthiobenzoyl)ferrocenes. Crystal structures of 2-methylthio, 2-ethylthio and 2-isopropylthio derivatives
Ratkovi?, Zoran,Novakovi?, Sladana B.,Bogdanovi?, Goran A.,?egan, Dejan,Vuki?evi?, Rastko D.
, p. 2311 - 2317 (2010/09/06)
The one-pot synthesis of seven new (2-alkylthiobenzoyl)ferrocenes has been achieved by Friedel-Crafts acylation of ferrocene with acid chlorides generated in situ from the corresponding carboxylic acids and phosphorous trichloride. The obtained compounds
PAN-ANTAGONISTS FOR THE ANDROGEN RECEPTOR AND ANDROGEN RECEPTOR MUTANTS ASSOCIATED WITH ANTI-ANDROGEN WITHDRAWAL
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Figure 42, (2008/06/13)
Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriat
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2, 1-a]isoindol-6(2H)-one, a selective, orally active agonist of the 5-HT 2C receptor
Wacker, Dean A.,Varnes, Jeffrey G.,Malmstrom, Sarah E.,Cao, Xueying,Hung, Chen-Pin,Ung, Thao,Wu, Ginger,Zhang, Ge,Zuvich, Eva,Thomas, Michael A.,Keim, William J.,Cullen, Mary Jane,Rohrbach, Kenneth W.,Qu, Qinling,Narayanan, Rangaraj,Rossi, Karen,Janovitz, Evan,Lehman-McKeeman, Lois,Malley, Mary F.,Devenny, James,Pelleymounter, Mary Ann,Miller, Keith J.,Robl, Jeffrey A.
, p. 1365 - 1379 (2007/10/03)
Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the synthesis and optimization of a new class of pyrazinoisoindolone- containing, selective 5-HT2C agonists as antiobesity agents. Key to optimization of the pyrazinoisoindolone core was the identification of the appropriate substitution pattern and functional groups which led to the discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a] isoindol-6(2H)-one (58), a 5-HT2C agonist with > 300-fold functional selectivity over 5-HT2B and > 70-fold functional selectivity over 5-HT2A. Oral dosing of 58 reduced food intake in an acute rat feeding model, which could be completely reversed by a selective 5-HT2C antagonist and caused a reduction in body weight gain in a 4-day rat model.
NOVEL COMPOUNDS
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Page/Page column 42, (2008/06/13)
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, - C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4/sub
Flash vacuum pyrolysis of stabilised phosphorus ylides. Part 12. Extrusion of Ph3P from sulfonyl ylides and reactivity of the resulting sulfonyl carbenes
Aitken, R. Alan,Drysdale, Martin J.,Ferguson, George,Lough, Alan J.
, p. 875 - 880 (2007/10/03)
Twelve sulfonyl stabilised phosphorus ylides have been prepared and their behaviour upon flash vacuum pyrolysis at 600°C has been examined. Examples with an arylsulfonyl substituent undergo loss of Ph3PO to give intractable products but those with an arylmethylsulfonyl substituent separately lose Ph3P and SO2 to give products consistent with the intermediacy of sulfonyl carbenes. X-Ray structure determinations of one ylide from each series show a more significant P-O non-bonding interaction in the first case, providing some explanation for the different thermal reactivity.
Flash vacuum pyrolysis of stabilised phosphorus ylides. Part 14. Tandem cyclisation of intermediate aryloxy and arylthio radicals leading to tri- and tetra-cyclic aromatic heterocycles
Aitken, R. Alan,Burns, Graham,Morrison, John J.
, p. 3937 - 3941 (2007/10/03)
Seven new stabilised phosphorus ylides 8-14 designed to undergo thermal tandem cyclisation have been prepared. Upon flash vacuum pyrolysis at 850°C, loss of Ph3PO and Me? results in tandem cyclisation to give benzothieno[3,2-b]benzothiophene 16 in the case of 11 while for 8 an abstraction-rearrangement-extrusion sequence leads to 2-phenylbenzofuran 18. For 9 and 10 both types of process occur to give respectively benzothieno[3,2-b]benzofuran 27, prepared here for the first time, and 2-phenylbenzothiophene 29. For 12 and 13, initial cyclisation is followed by intramolecular addition and aromatisation to give the tricyclic products 31 and 32, while for 14 intramolecular homolytic substitution leads to the tetracyclic benzonaphthofuran 34 and, by rearrangement, to the isomer 37. Fully assigned 13C NMR spectra are presented for all seven ylides.
Synthesis of pyrazolo[1,5-b][1,2]benzisothiazoles
Moyroud, Joel,Chene, Alain,Guesnet, Jean-Luc,Mortier, Jacques
, p. 221 - 228 (2007/10/02)
The synthesis of some pyrazolo[1,5-b] [1,2]benzisothiazoles is described. The route is based on the reaction between 3(5)-[2′-methylthiophenyl]pyrazoles and its derivatives with N-chlorosuccinimide.
