- REACTIONS OF SULPHURYL FLUORIDE, SULPHURYL CHLOROFLUORIDE AND SULPHURYL CHLORIDE WITH AMINES
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The reactions of sulphuryl fluoride, sulphuryl chlorofluoride and sulphuryl chloride with the amines tert-butylamine, benzylamine, piperidine, pyridine and quinoline have been investigated.The primary and secondary amines react with the elimination of hydrogen halides and formation of S-N bonds whereas tertiary amines form 1:2 adducts.
- Padma, D. K.,Bhat, V. Subrahmanya,Murthy, A. R. Vasudeva
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- Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors
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p53-MDM2/MDMX interaction inhibitors represent the prospective agents for targeted anticancer therapy in tumors expressing wild-type p53 protein. Imidazoline-based MDM2-targeted inhibitors of such type, nutlins, contain halogen-substituted phenyl rings, w
- Bazanov, Daniil R.,Kopeina, Gelina S.,Lozinskaya, Natalia A.,Maksutova, Anita I.,Pervushin, Nikolay V.,Savin, Egor V.,Sosonyuk, Sergey E.,Tsymliakov, Michael D.
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p. 2216 - 2227
(2021/10/14)
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- Nickel-Catalyzed Hydrodeoxygenation of Aryl Sulfamates with Alcohols as Mild Reducing Agents
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The nickel-catalyzed hydrodeoxygenation of aryl sulfamates has been developed with alcohols as mild reductants. A variety of functional groups and heterocycles were tolerated in this reaction system to give the desired products in high yields. In addition, the gram-scale process and stepwise cine-substitution were also achieved with high efficiency.
- Matsuo, Kasumi,Kuriyama, Masami,Yamamoto, Kosuke,Demizu, Yosuke,Nishida, Koyo,Onomura, Osamu
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p. 4449 - 4460
(2021/08/25)
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- S(vi) in three-component sulfonamide synthesis: Use of sulfuric chloride as a linchpin in palladium-catalyzed Suzuki-Miyaura coupling
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Sulfuric chloride is used as the source of the -SO2- group in a palladium-catalyzed three-component synthesis of sulfonamides. Suzuki-Miyaura coupling between the in situ generated sulfamoyl chlorides and boronic acids gives rise to diverse sulfonamides in moderate to high yields with excellent reaction selectivity. Although this transformation is not workable for primary amines or anilines, the results show high functional group tolerance. With the solving of the desulfonylation problem and utilization of cheap and easily accessible sulfuric chloride as the source of sulfur dioxide, redox-neutral three-component synthesis of sulfonamides is first achieved. This journal is
- Wang, Xuefeng,Yang, Min,Ye, Shengqing,Kuang, Yunyan,Wu, Jie
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p. 6437 - 6441
(2021/05/19)
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- Triazole compounds and their use in agriculture (by machine translation)
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The present invention provides a triazole compound and its application in agriculture; in particular, the invention provides compounds of formula (A) indicated by the compound and its preparation method; the composition containing these compounds and preparation and their use as fungicides; wherein R1 , R2 , R3 , W, R4 , R5 , R6 , R7 , R8 , R9 , Ra , Rb And in the event of x has the meanings given by the invention. (by machine translation)
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Paragraph 0438; 0439; 0440; 0442; 0444
(2018/11/04)
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- PREPARATION OF COBICISTAT INTERMEDIATES
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The present disclosure provides crystalline piperidine sulfamoyl intermediates of formula 8 and 9. The present disclosure also relates to an improved process for the preparation of cobicistat using compounds of formulae 8 and 9.
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Page/Page column 11-12
(2015/06/18)
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- Synthesis of aryl sulfonamides via palladium-catalyzed chlorosulfonylation of arylboronic acids
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A palladium-catalyzed method for the preparation of sulfonamides is described. The process exhibits significant functional group tolerance and allows for the preparation of a number of arylsulfonyl chlorides and sulfonamides under mild conditions.
- Debergh, J. Robb,Niljianskul, Nootaree,Buchwald, Stephen L.
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p. 10638 - 10641
(2013/08/23)
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- OXYCARBAMOYL COMPOUNDS AND THE USE THEREOF
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The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockadeof calcium channels, and particularly N-type calcium channe
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Page/Page column 89
(2010/01/07)
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- Inhibitors of HCV NS5B polymerase: Synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides
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Substituted N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides were investigated as inhibitors of genotype 1 HCV polymerase. Structure-activity relationship patterns for this class of compounds are discussed.
- Chris Krueger,Madigan, Darold L.,Jiang, Wen W.,Kati, Warren M.,Liu, Dachun,Liu, Yaya,Maring, Clarence J.,Masse, Sherie,McDaniel, Keith F.,Middleton, Tim,Mo, Hongmei,Molla, Akhteruzzaman,Montgomery, Debra,Pratt, John K.,Rockway, Todd W.,Zhang, Rong,Kempf, Dale J.
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p. 3367 - 3370
(2007/10/03)
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- NOVEL COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE
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The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
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Page/Page column 81-82
(2010/02/14)
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- Potent and selective, sulfamide-based human β3-adrenergic receptor agonists
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A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human β3- adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintai
- Dow, Robert L.,Paight, Ernest S.,Schneider, Steven R.,Hadcock, John R.,Hargrove, Diane M.,Martin, Kelly A.,Maurer, Tristan S.,Nardone, Nancy A.,Tess, David A.,DaSilva-Jardine, Paul
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p. 3235 - 3240
(2007/10/03)
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- Sulfonamide inhibitors of aspartyl protease
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The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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- SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
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The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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- Oestrone 3-O-(N-acetyl)sulphamate, a potential molecular probe of the active site of oestrone sulphatase
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N,N-Dialkylated derivatives of the steroid sulphatase inhibitor, oestrone 3-O-sulphamate (EMATE) are weak reversible inhibitors of the enzyme. N-Acetylated-EMATE (8), but not the benzoyl derivative, inhibits the enzyme irreversibly, albeit less potently than EMATE and will allow hitherto difficult radiolabelling on the sulphamate group to facilitate investigation of the enzyme inactivation mechanism.
- Woo, L. W. Lawrence,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
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p. 3075 - 3080
(2007/10/03)
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- SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
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The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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- BASICITY OF NITROGEN-SULPHUR(VI) COMPOUNDS. PART 5. IONIZATION OF TRISUBSTITUTED SULPHAMIDES
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The ionization equilibria in base of 27 trisubstituted sulphamides, mainly represented by the following series: X-C6H4NHSO2NR2R1, where NR2R1=piperidyl, morpholinyl, and NnPr2, and RHNSO2NR2R1/s
- McDermott, Sean D.,Burke, Padraig O.,Spillane, William J.
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p. 499 - 502
(2007/10/02)
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