- COMPOUNDS AS NEUROKININ-1 RECEPTOR ANTAGONISTS AND USES THEREOF
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The present invention relates compounds of Formula (A) as NK-1 receptor antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate
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Page/Page column 42-43
(2020/02/16)
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- Five sulfur hexafluoride substituted benzo-type compounds and use thereof
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The invention discloses a sulfur pentafluoride-substituted benzopyran compound shown in the structural formula I or its pharmaceutically acceptable salt or stereoisomer or prodrug molecule. The sulfur pentafluoride-substituted benzopyran compound has effe
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Paragraph 0118; 0120; 0121
(2018/10/11)
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- UREA DERIVATIVE AND USE THEREFOR
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The purpose of the present invention is to provide a compound with inhibitory activity on Discoidin Domain Receptor 1. The present invention provides a urea derivative represented by the formula (I) below or a pharmaceutically acceptable salt thereof.
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Paragraph 0208; 0209
(2018/07/29)
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- UREA DERIVATIVE AND USE THEREFOR
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The purpose of the present invention is to provide a compound with inhibitory activity on Discoidin Domain Receptor 1. The present invention provides a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof.
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Paragraph 0220
(2018/07/29)
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- Pentafluorosulfanyl-Substituted Benzopyran Analogues As New Cyclooxygenase-2 Inhibitors with Excellent Pharmacokinetics and Efficacy in Blocking Inflammation
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In this report, we disclose the design and synthesis of a series of pentafluorosulfanyl (SF5) benzopyran derivatives as novel COX-2 inhibitors with improved pharmacokinetic and pharmacodynamic properties. The pentafluorosulfanyl compounds showe
- Zhang, Yanmei,Wang, Yican,He, Chuang,Liu, Xiaorong,Lu, Yongzhi,Chen, Tingting,Pan, Qiong,Xiong, Jingfang,She, Miaoqin,Tu, Zhengchao,Qin, Xiaochu,Li, Minke,Tortorella, Micky D.,Talley, John J.
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p. 4135 - 4146
(2017/06/05)
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- Synthesis of 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate and analogs and their application for the preparation of SF5-aromatics
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4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate salt was synthesized and isolated. The pentafluorosulfanyl salt was examined in a wide assortment of reactions to form novel SF5-bearing alkenes, alkynes, and biaryl derivatives using Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation of the salt furnished the corresponding p-SF5—C6H4X,C6H4OS(O)(CF3)═NSO2CF3, and p-SF5—C6H4-NTf2 derivatives. The azide derivative p-SF5—C6H4N3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. Various SF5-bearing alkenes were synthesized by coupling reactions using a metal catalyst. Fluorodediazoniation selectively furnished the fluoro derivative p-SF5—C6H4F. Homolytic dediazoniation gave the unsymmetrical biaryls, thus demonstrating the broad utility of pentafluorosulfanyl diazonium salts as building blocks of SF5-aromatics that are in high demand in many branches of chemistry including biomedicine and materials chemistry.
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- 4-(Pentafluorosulfanyl)benzenediazonium Tetrafluoroborate: A Versatile Launch Pad for the Synthesis of Aromatic SF5 Compounds via Cross Coupling, Azo Coupling, Homocoupling, Dediazoniation, and Click Chemistry
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The reagent 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate (1) was synthesized and isolated as a stable salt for the first time; its application in a wide assortment of transformations was subsequently investigated. A series of novel SF5-bearing alkenes, alkynes, and biaryl derivatives were synthesized by employing Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation with TMSX (X = Hal; N3; and CN) and NH4SCN in [BMIM][BF4] as solvent furnished the corresponding p-SF5-C6H4X derivatives. The azide derivative p-SF5-C6H4N3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. The 4,4′-bis(pentafluorosulfanyl)biphenyl was synthesized by homo-coupling using Pd(OAc)2. The corresponding azo compounds were obtained through azo-coupling with reactive aromatic nucleophiles (1,3-dimethoxybenzene, 1,3,5-trimethoxybenzene, 1,2,4-trimethoxybenzene, aniline and phenol). Fluorodediazoniation in [BMIM][PF6] and [BMIM][BF 4] selectively furnished the fluoro derivative p-SF 5-C6H4F. Dediazoniation in [BMIM][NTf 2] gave p-SF5-C6H4OS(O)(CF 3)=NSO2CF3 as the major and p-SF 5-C6H4-NTf2 as the minor products. Homolytic dediazoniation in MeCN/NaI gave the unsymmetrical biaryls p-SF 5-C6H4-Ar (ArH = mesitylene and p-xylene) along with p-SF5-C6H4I. Analysis of the dediazoniation product mixtures indicated that dediazoniation of p-SF 5-C6H4N2+ BF 4- in low nucleophilicity, highly ionizing, solvents (TfOH, TFE, HFIP, TFAH) is mainly heterolytic, while in MeOH it is mainly homolytic. The isodesmic reaction p-SF5-C6H 4+ + R-C6H5 → SF 5-C6H5 + p-R-C6H4 + (with R = NO2, CF3, H) was gauged by DFT at various levels and by PCM. Copyright
- Okazaki, Takao,Laali, Kenneth K.,Bunge, Scott D.,Adas, Sonya K.
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p. 1630 - 1644
(2014/03/21)
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- 4-(Pentafluorosulfanyl)benzenediazonium Tetrafluoroborate: A Versatile Launch Pad for the Synthesis of Aromatic SF5 Compounds via Cross Coupling, Azo Coupling, Homocoupling, Dediazoniation, and Click Chemistry
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The reagent 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate (1) was synthesized and isolated as a stable salt for the first time; its application in a wide assortment of transformations was subsequently investigated. A series of novel SF5-bearing alkenes, alkynes, and biaryl derivatives were synthesized by employing Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation with TMSX (X = Hal; N3; and CN) and NH4SCN in [BMIM][BF4] as solvent furnished the corresponding p-SF5-C6H4X derivatives. The azide derivative p-SF5-C6H4N3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. The 4,4′-bis(pentafluorosulfanyl)biphenyl was synthesized by homo-coupling using Pd(OAc)2. The corresponding azo compounds were obtained through azo-coupling with reactive aromatic nucleophiles (1,3-dimethoxybenzene, 1,3,5-trimethoxybenzene, 1,2,4-trimethoxybenzene, aniline and phenol). Fluorodediazoniation in [BMIM][PF6] and [BMIM][BF4] selectively furnished the fluoro derivative p-SF5-C6H4F. Dediazoniation in [BMIM][NTf2] gave p-SF5-C6H4OS(O)(CF3)=NSO2CF3 as the major and p-SF5-C6H4-NTf2 as the minor products. Homolytic dediazoniation in MeCN/NaI gave the unsymmetrical biaryls p-SF5-C6H4-Ar (ArH = mesitylene and p-xylene) along with p-SF5-C6H4I. Analysis of the dediazoniation product mixtures indicated that dediazoniation of p-SF5-C6H4N2+ BF4- in low nucleophilicity, highly ionizing, solvents (TfOH, TFE, HFIP, TFAH) is mainly heterolytic, while in MeOH it is mainly homolytic. The isodesmic reaction p-SF5-C6H4+ + R-C6H5 → SF5-C6H5 + p-R-C6H4+ (with R = NO2, CF3, H) was gauged by DFT at various levels and by PCM.
- Okazaki, Takao,Laali, Kenneth K.,Bunge, Scott D.,Adas, Sonya K.
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p. 1630 - 1644
(2015/10/05)
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- Synthesis of aliphatic sulfur pentafluorides by oxidation of SF5-containing anisole, phenols, and anilines
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4-(Pentafluorosulfanyl)catechol, 2-amino-4-(pentafluorosulfanyl)phenol, and 2-amino-5-(pentafluorosulfanyl) phenol undergo oxidation by lead tetraacetate at ambient temperature leading to dearomatization and the formation of SF5-substituted nit
- Vida, Norbert,Pastkov, Tereza,Klepetov, Blanka,Beier, Petr
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p. 8906 - 8911
(2015/01/08)
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- PROCESS FOR THE PREPARATION OF 3- AND 4-(PENTAFLUOROSULFANYL)BENZENES
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Process for the preparation of substituted 3- and 4-(pentafluorosulfanyI)benzenes of general formula 3 and 4 by nucleophilic aromatic substitution, where nitrobenzene having pentafiuorosulfanyl group connected in position 3 or 4 is allowed to react in concentration range 0.01 to 8.0 mol.l-1 with compound RY-M+, where R is selected from a group comprising saturated, unsaturated, acyclic, cyclic or aromatic, substituted or unsubstituted carbon chain, Y is the element of VI. B group and M+ is the metal ion, in an organic solvent. The invention includes also further chemical modifications of primary products.
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Page/Page column 10; 11
(2012/04/23)
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- SNAr reactions of nitro-(pentafluorosulfanyl)benzenes to generate SF5 aryl ethers and sulfides
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Nucleophilic aromatic substitution of the nitro group of para- and meta-nitro-(pentafluorosulfanyl)benzene with alkoxides and thiolates generates a range of substituted 4- and 3-(pentafluorosulfanyl)benzenes in a single-step reaction.
- Beier, Petr,Pastyrikova, Tereza,Vida, Norbert,Iakobson, George
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supporting information; experimental part
p. 1466 - 1469
(2011/06/09)
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- ORTHO-SUBSTITUTED PENTAFLUORIDE SULFANYL-BENZENES, METHOD FOR THE PRODUCTION THEREOF AND THE USE THEREOF IN THE FORM OF VALUABLE SYNTHESIS INTERMEDIATE STAGES
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The invention relates to pentafluoride-sulfanyl-benzenes of formula (I), wherein groups from R1 to R5 correspond to meanings given in claims and constitute valuable intermediates, for example for producing drugs, diagnosis agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
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Page/Page column 33
(2010/02/11)
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