- NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
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The present invention relates to a new compound having an FGFR inhibitory activity and preparation and application thereof. In particular, the compound according to the present invention has a structure as shown in formula I, wherein each group and substituent are as defined in the description. Also disclosed in the present invention are a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease.
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Paragraph 0112; 0113; 0114
(2019/05/30)
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- Controlling the Course of a Two-Way Switchable Pd-Catalyzed Process by means of Empirical Multivariate Models
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A two-way switchable Pd-catalyzed process that can pursue two different mechanisms, namely hydro- and methoxy-deiodination was discovered, developed, and optimized by means of statistical experimental design, multivariate modelling, and response surface methodology. The investigation revealed that the two-way switchable process might be controlled either by ligand alone, or by ligand and other process variables in combination. The present study represents the first example of a catalytic system that provides either hydro- or methoxy-deiodination selectively by simply fine-tuning the experimental variables.
- Sandtorv, Alexander H.,Bj?rsvik, Hans-René
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p. 2196 - 2205
(2015/11/24)
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- A tandem reduction-oxidation protocol for the conversion of 1-keto-1,2,3,4-tetrahydrocarbazoles to carbazoles via tosylhydrazones through microwave assistance: Efficient synthesis of glycozoline, clausenalene, glycozolicine, and deoxycarbazomycin B and the total synthesis of murrayafoline A
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A novel and efficient methodology for the synthesis of carbazoles from 1-keto-1,2,3,4-tetrahydrocarbazoles via the corresponding tosylsulfonhydrazones by a one-pot tandem reduction-oxidation protocol using a combination of NaBH4 and Pd-C on MgSO4·7H2O, a solid support, under microwave is developed. The reaction is successfully extended toward the synthesis of several naturally occurring carbazole alkaloids, namely 3-methylcarbazole, glycozoline, clausenalene, glycozolicine, murrayafoline A, and deoxycarbazomycin B, a carbazole derivative that is known to have a promising antimicrobial activity.
- Chakraborty, Suchandra,Chattopadhyay, Gautam,Saha, Chandan
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- Acid-free synthesis of carbazoles and carbazolequinones by intramolecular Pd-catalyzed, microwave-assisted oxidative biaryl coupling reactions efficient syntheses of murrayafoline A, 2-methoxy-3-methylcarbazole, and glycozolidine
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A mild and. efficient methodology for the synthesis of oxygenated. carbazoles from diarylamines under non-acidic conditions was developed, based on a palladium-catalyzed, microwave-assisted double C-H bond activation process. This new protocol was successfully applied to the synthesis of three naturally occurring carbazoles, namely murrayafoline A, 2-methoxy-3-methylcarbazole, and glycozolidine. The scope of the reaction was also expanded, to include the synthesis of benzo fused carbazolequinones. Wiley-VCH Verlag GmbH & Co. KGaA.
- Sridharan, Vellaisamy,Antonia Martin,Carlos Menendez
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supporting information; experimental part
p. 4614 - 4621
(2009/12/05)
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- COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACIDS AND POLYPEPTIDES
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Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.
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Page/Page column 172; 12/40
(2008/06/13)
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- Synthesis of oxygenated carbazoles by palladium-mediated oxidative double C-H activation of diarylamines assisted by microwave irradiation
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Microwave irradiation in the presence of palladium acetate and traces of dimethylformamide allows the fast and efficient cyclodehydrogenation of diphenylamines into carbazoles. The scope of the microwave-assisted reaction is broader than that of the one using conventional conditions in that it allows the preparation of oxygenated carbazoles without apparent loss in yield. The applicability of the method to the preparation of carbazole alkaloids has been demonstrated by the development of a total synthesis of murrayafoline A, which proceeds in 50% overall yield from commercially available materials and is the shortest and most efficient route for the preparation of this alkaloid to date. Georg Thieme Verlag Stuttgart.
- Sridharan, Vellaisamy,Martín, Ma. Antonia,Menéndez, J. Carlos
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p. 2375 - 2378
(2008/02/09)
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- Separated and Aligned Molecular Fibres in Solid State Self-Assemblies of Cyclodextrin [2]Rotaxanes
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The conformations of two [2]rotaxanes, each comprising α -cyclodextrin as the rotor, a stilbene as the axle and 2,4,6-trinitrophenyl substituents as the capping groups, have been examined in solution and in the solid state, using 1H NMR spectroscopy and X-ray crystallography, respectively. In solution, introducing substituents onto the stilbene prevents the cyclodextrin from being localized over one end of the axle. Instead the cyclodextrin moves back and forth along the substituted stilbene. In the solid state, the axles of the rotaxanes form extended molecular fibres that are separated from each other and aligned along a single axis. The molecular fibres are strikingly similar to those formed by the axle component of one of the rotaxanes in the absence of the cyclodextrin, but in the latter case they are neither separated nor all aligned.
- Onagi, Hideki,Carrozzini, Benedetta,Cascarano, Giovanni L.,Easton, Christopher J.,Edwards, Alison J.,Lincoln, Stephen F.,Rae, A. David
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p. 5971 - 5977
(2007/10/03)
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- N-Arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective α1-adrenoceptor antagonists
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Novel arylpiperazines were identified as α1-adrenoceptor (AR) subtype- selective antagonists by functional in vitro screening. 3-[4-(ortho- Substituted phenyl)piperazin-1:yl]propylamines were derivatized with N,N- dimethyl anthranilamides, nicotinamides, as well as carboxamides of quinoline, 1,8-naphthyridine, pyrazolo[3,4-b]pyridine, isoxazolo[3,4- b]pyridine, imidazo[4,5-b]pyridine, and pyrazolo[1,5-a]pyrimidines. Strips of rabbit bladder neck were employed as a predictive assay for antagonism in the human lower tract. Rings of rat aorta were used as a 'negative screen' for the test antagonists. Binding to α1-ARs was relatively sensitive to size and electronic features of the arylpiperazine portion of the antagonists and permissive to these features on the heteroaryl carboxamide side. These structure-affinity findings were exploited to produce nicotinamides (e.g. 13ii and 25x) and pyrazolo[3,4-b]pyridines (e.g. 37f and 37y) ligands with nanomolar affinity at the α1-AR subtype prevalent in the human lower urinary tract (pA2 values: 8.8, 10.7, 9.3, and 9.9, respectively) and displaying 2-3 orders of magnitude selectivity over the α(1D)-AR.
- Elworthy, Todd R.,Ford, Anthony P. D. W.,Bantle, Gary W.,Morgans Jr., David J.,Ozer, Rachel S.,Palmer, Wylie S.,Repke, David B.,Romero, Magarita,Sandoval, Leticia,Sjogren, Eric B.,Talamás, Francisco X.,Vazquez, Alfredo,Wu, Helen,Arredondo, Nicolas F.,Blue Jr., David R.,DeSousa, Andrea,Gross, Lisa M.,Kava, M. Shannon,Lesnick, John D.,Vimont, Rachel L.,Williams, Timothy J.,Zhu, Quan-Ming,Pfister, Jürg R.,Clarke, David E.
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p. 2674 - 2687
(2007/10/03)
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- 13C NMR Spectra of Substituted o-Nitroanisoles and n-Butyl o-Nitrophenyl Ethers
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13C NMR analyses of substituted o-nitroanisoles and n-butyl o-nitrophenyl ethers are reported. Key Words: 13C NMR - o-Nitroanisoles - n-Butyl o-nitrophenyl ethers
- Zeegers, Petrus J.,Thompson, Malcolm J.
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p. 497 - 499
(2007/10/02)
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- Interaction between Electron Donor and Acceptor Groups in Some Trisubstituted Benzenes. Part 1. Relative Reactivities of 4-Substituted 1,2-Dinitrobenzenes towards Sodium Methoxide
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In an effort to study the effects of 'through conjugation' on the properties of some 1,2,4-trisubstituted benzenes, the rates of reaction of a series of four 4-substituted 1,2-dinitrobenzenes with sodium methoxide in methanol have been studied.Although reactivities at the 2-position were qualitatively in the order to be expected from inductive effects, those at the 1-position were highly sensitive to the influence of mesomeric donor action of the 4-substituent.Relatively large effects were seen for the 4-alkyl derivatives; and C-H hyperconjugation appeared to be stronger than C-C hyperconjugation.
- Patil, Sampatrao D.,Nair, P. Madhavan
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p. 637 - 640
(2007/10/02)
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- Naturally Occurring Dibenzofurans. Part 5. Synthesis of Melacarpic Acid
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The total synthesis of the lichen dibenzofuran melacarpic acid (5) was achieved by intramolecular Ullman coupling of methyl 5-bromo-4-(2-bromo-5-methoxy-3-methylphenoxy)-6-heptyl-2-methoxybenzoate (48) or methyl 6-heptyl-5-iodo-4-(2-iodo-5-methoxy-3-methyl-4-nitrophenoxy)-2-methoxybenzoate (46) followed by appropriate transformations.
- Carvalho, Christopher F.,Sargent, Melvyn V.
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p. 1613 - 1620
(2007/10/02)
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- Nitration in Aqueous Nitric Acid: the Rate Profile and the Limiting Reaction Rates
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Rate coefficients for the nitration of a series of quaternary ammonium ions have been used to establish a rate profile for reaction in 63.7percent-100percent nitric acid at 25 deg C and to estimate the concentration of nitronium ions in the aqueous media.The kinetics of nitration of a series of reactive aromatic aromatic compounds (mainly phenolic ethers) in aqueous nitric acid have been analysed in terms of a first-order rate coefficient and the zeroth-order rate of formation of the nitronium ion.The first-order rate coefficients approach a limiting value as the reactivity of the aromatic substrate is increased and this value is as expected for the rate-limiting formation of an encounter pair (ArH*NO2+).The lifetime of nitronium ions in 60.4percent nitric acid (t1/2 ca. 5 x 10-8 s) has been calculated from the zeroth-order rate at 25 deg C and used to show that the formation of the encounter pair (ArH*NO2+) occurs by the diffusion together of the components, not by pre-association.The studies on the more reactive aromatic compounds were carried out in the presence of hydrazine since this was shown to prevent the nitrous-acid catalysed reactions previously observed.
- Draper, Mark R.,Ridd, John H. A.
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- Synthesis of Benzothiazoles. α-Amino-(4-hydroxy-6-benzothiazolyl)propionic Acid.
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The tentative structure assigned to the photobiologically important skin pigment pheomelanin is based on degradative studies of the natural chromophore.The title compound was reported to be one of several key amino acids isolated in these studies.The identity of this benzothiazole derivative has now been confirmed via an unambiguous eight-step total synthesis starting from 5-methyl-2-nitrophenol.
- Ismail, Ibrahim A.,Sharp, Dale E.,Chedekel, Miles R.
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p. 2243 - 2246
(2007/10/02)
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- Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogues
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A series of melatonin analogues was synthesized and examined for ovulation-blocking activity. Deviation from the 5-methoxy group or substitution of the 1 position prevented activity. Activity was not particularly sensitive to minor variations in the N-acyl group nor was it significantly altered by methylation of position 2 or the α-methylene; however, a pronounced enhancement resulted from halogenation of the 6 position.
- Flaugh,Crowell,Clemens,Sawyer
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