64080-15-5Relevant academic research and scientific papers
Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use
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Paragraph 2276, (2019/03/30)
The invention discloses compounds of Formula (I), wherein A1, R1, R2, R3, R4, and n are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
Trifluoromethyl aryl sulfonates (TFMS): An applicable trifluoromethoxylation reagent
Lei, Meng,Miao, Hang,Wang, Xueyuan,Zhang, Wen,Zhu, Chengjian,Lu, Xiaqiang,Shen, Jian,Qin, Yanru,Zhang, Haoyang,Sha, Sijia,Zhu, Yongqiang
supporting information, p. 1389 - 1392 (2019/04/30)
Fluorine is probably another favorite hetero-atom for incorporation into small molecules after nitrogen. Among many fluorine-containing groups, trifluoromethyl aryl ethers (ArOCF3) have unique properties in drug design and are difficult to be synthesized, and many different methods were developed to prepare them. A novel one-pot synthesis of o-iodine-aryl trifluoromethyl ethers (ArOCF3I) was described by the reaction of trifluoromethoxylation and iodination with trifluoromethyl aryl sulfonates (TFMS) in this manuscript. The reaction conditions were optimized by screening different solvents, crown ethers, substrates and the ratios and the yields of products were in moderate to high yields (up to 86%).
Expedient Access to 2-Benzazepines by Palladium-Catalyzed C?H Activation: Identification of a Unique Hsp90 Inhibitor Scaffold
Virelli, Matteo,Moroni, Elisabetta,Colombo, Giorgio,Fiengo, Lorenzo,Porta, Alessio,Ackermann, Lutz,Zanoni, Giuseppe
supporting information, p. 16516 - 16520 (2018/10/25)
Bioactive 2-benzazepines were accessed in an atom- and step-economical manner through a versatile palladium-catalyzed C?H activation strategy. The C?H arylation required low catalyst loading and a mild base, which was reflected by a broad scope and high functional-group tolerance. The benzotriazolodiazepinones were identified as new heat shock protein 90 (Hsp90) inhibiting lead compounds, with considerable potential for anti-cancer applications.
Indanol-Based Chiral Organoiodine Catalysts for Enantioselective Hydrative Dearomatization
Hashimoto, Takuya,Shimazaki, Yuto,Omatsu, Yamato,Maruoka, Keiji
supporting information, p. 7200 - 7204 (2018/06/15)
Rapid development in the last decade has rendered chiral organoiodine(I/III) catalysis a reliable methodology in asymmetric catalysis. However, due to the severely limited numbers of effective organoiodine catalysts, many reactions still give low to modes
Palladium-catalyzed paraformaldehyde insertion: A three-component synthesis of benzofurans
Cheng, Xiufang,Peng, Yi,Wu, Jun,Deng, Guo-Jun
supporting information, p. 2819 - 2823 (2016/03/12)
An efficient procedure for 2-aroylbenzofuran preparation from 2-bromophenols, phenacyl bromides and paraformaldehyde is described. The cheap and stable paraformaldehyde served as the carbon source via an in situ formylation reaction.
Structural analogues of the natural products magnolol and honokiol as potent allosteric potentiators of GABAA receptors
Fuchs, Alexander,Baur, Roland,Schoeder, Clara,Sigel, Erwin,Müller, Christa E.
supporting information, p. 6908 - 6917 (2015/02/02)
Biphenylic compounds related to the natural products magnolol and 4′-O-methylhonokiol were synthesized, evaluated and optimized as positive allosteric modulators (PAMs) of GABAA receptors. The most efficacious compounds were the magnolol analog 5-ethyl-5′-hexylbiphenyl-2,2′-diol (45) and the honokiol analogs 4′-methoxy-5-propylbiphenyl-2-ol (61), 5-butyl-4′-methoxybiphenyl-2-ol (62) and 5-hexyl-4′-methoxybiphenyl-2-ol (64), which showed a most powerful potentiation of GABA-induced currents (up to 20-fold at a GABA concentration of 3 μM). They were found not to interfere with the allosteric sites occupied by known allosteric modulators, such as benzodiazepines and N-arachidonoylglycerol. These new PAMs will be useful as pharmacological tools and may have therapeutic potential for mono-therapy, or in combination, for example, with GABAA receptor agonists.
METHYLPYRROLOPYRIMIDINECARBOXAMIDES
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Page/Page column 104, (2012/06/18)
The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
METHYLPYRROLOPYRIMIDINECARBOXAMIDES
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Page/Page column 166-167, (2011/04/14)
The compounds of formula (I) wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, and the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiestera
A simple synthetic protocol for oxidation of alkyl-arenes into ketones using a combination of HBr-H2O2
Khan, Abu T.,Parvin, Tasneem,Choudhury, Lokman H.,Ghosh, Subrata
, p. 2271 - 2274 (2007/10/03)
A wide variety of alkyl- and cycloalkyl-arenes undergo benzylic C-H oxidation by employing a combination of 48% hydrogen bromide and 30% hydrogen peroxide in dichloromethane at room temperature. In addition, a chemoselective oxidation at the benzylic position is feasible by deactivating the aromatic ring using the same combination.
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
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Page/Page column 169-170, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
