- B(C6F5)3-Catalyzed C-H Alkylation of N-Alkylamines Using Silicon Enolates without External Oxidant
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An efficient method for the coupling of N-alkylamines with silicon enolates to generate β-amino carbonyl compounds is disclosed. These reactions proceed by activation of α-amino C-H bonds by B(C6F5)3, which likely generate
- Chan, Jessica Z.,Chang, Yejin,Wasa, Masayuki
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supporting information
p. 984 - 988
(2019/02/14)
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- C-H Functionalization of Amines via Alkene-Derived Nucleophiles through Cooperative Action of Chiral and Achiral Lewis Acid Catalysts: Applications in Enantioselective Synthesis
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Catalytic transformations of α-amino C-H bonds to afford valuable enantiomerically enriched α-substituted amines, entities that are prevalent in pharmaceuticals and bioactive natural products, have been developed. Typically, such processes are carried out
- Shang, Ming,Chan, Jessica Z.,Cao, Min,Chang, Yejin,Wang, Qifan,Cook, Brennan,Torker, Sebastian,Wasa, Masayuki
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supporting information
p. 10593 - 10601
(2018/08/03)
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- PYRAZOLOPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR USE IN PREVENTING OR TREATING CANCER, AUTOIMMUNE DISEASE AND BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.
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Paragraph 628-632
(2018/12/02)
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- SULFONAMIDES AS GPR40- AND GPR120-AGONISTS
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The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I). Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabet
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Page/Page column 22
(2018/03/06)
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- Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions
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Herein, we describe the development of copper-catalyzed cross-coupling of DNA-conjugated aryl iodides with aliphatic amines. This protocol leverages a novel ligand, 2-((2,6-dimethoxyphenyl)amino)-2-oxoacetic acid, to effect the transformation in aqueous D
- Ruff, Yves,Berst, Frédéric
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supporting information
p. 1188 - 1193
(2018/08/01)
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- Selective Cross-Coupling of (Hetero)aryl Halides with Ammonia to Produce Primary Arylamines using Pd-NHC Complexes
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Herein we report the first example of (hetero)arylation of ammonia using a monoligated palladium-NHC complex. The new, rationally designed, precatalyst (DiMeIHeptCl)Pd(allyl)Cl featuring highly branched alkyl chains has been shown to be effective in selective aminations across a range of challenging substrates, including nitrogen-containing heterocycles and those featuring base-sensitive functionality. The less bulky Pd-PEPPSI-IPentCl precatalyst performs well for ortho-substituted aryl halides, giving monoarylated products in high yield with good selectivity.
- Lombardi, Christopher,Day, Jonathan,Chandrasoma, Nalin,Mitchell, David,Rodriguez, Michael J.,Farmer, Jennifer L.,Organ, Michael G.
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supporting information
p. 251 - 254
(2017/04/26)
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- PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
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The present invention discloses substituted pyrimidine and pyrimido indole compounds and optionally pharmaceutically acceptable salts, hydrates or solvates thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
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Page/Page column 51
(2016/03/19)
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- Synthesis of 1,2-diaryl- and 1-aryl-2-alkylimidazoles with sterically demanding substituents
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1,2-Diarylimidazoles are an important class of compounds. They are frequently used as ligands for photophysically active metal complexes and also display physiological activity. We developed a new, high-yielding procedure for the synthesis of 1,2-diaryl-s
- Micksch, Maik,Tenne, Mario,Strassner, Thomas
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p. 6137 - 6145
(2013/09/24)
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- Iron-catalyzed formation of 2-aminopyridines from diynes and cyanamides
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Diynes and cyanamides undergo an iron-catalyzed [2 + 2 + 2] cycloaddition to form highly substituted 2-aminopyridines in an atom-efficient manner that is both high yielding and regioselective. This system was also used to cyclize two terminal alkynes and
- Lane, Timothy K.,D'Souza, Brendan R.,Louie, Janis
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p. 7555 - 7563
(2012/11/07)
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- Substituent effects on aromatic stacking interactions
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Synthetic supramolecular zipper complexes have been used to quantify substituent effects on the free energies of aromatic stacking interactions. The conformational properties of the complexes have been characterised using NMR spectroscopy in CDCl3, and by comparison with the solid state structures of model compounds. The structural similarity of the complexes makes it possible to apply the double mutant cycle method to evaluate the magnitudes of 24 different aromatic stacking interactions. The major trends in the interaction energy can be rationalised using a simple model based on electrostatic interactions between the π-faces of the two aromatic rings. However, electrostatic interactions between the substituents of one ring and the π-face of the other make an additional contribution, due to the slight offset in the stacking geometry. This property makes aromatic stacking interactions particularly sensitive to changes in orientation as well as the nature and location of substituents. This journal is The Royal Society of Chemistry.
- Cockroft, Scott L.,Perkins, Julie,Zonta, Cristiano,Adams, Harry,Spey, Sharon E.,Low, Caroline M. R.,Vinter, Jeremy G.,Lawson, Kevin R.,Urch, Christopher J.,Hunter, Christopher A.
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p. 1062 - 1080
(2007/12/27)
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- HIV INHIBITING 1,2,4-TRIAZIN-6-ONE DERIVATIVES
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The present invention relates to HIV replication inhibitors of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridaz
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Page/Page column 55-56
(2008/06/13)
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- HIV INHIBITING 1,2,4-TRIAZINES
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The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
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- The Schmidt reaction of dialkyl acylphosphonates
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The scope of the Schmidt rearrangement of ketones has been extended to dialkyl acylphosphonates (11a-11l). Surprisingly, it was found that 11a-11d and 11g, in which the acyl moiety was benzoyl alone or benzoyl bearing an electron-attracting or mildly electron-releasing substituent, yielded an overwhelming portion of products resulting from C-to-N migration of the aryl group (N-arylcarbamoylphosphonates, 12, and N-arylformamides, 15). Contrariwise, the arenecarbonylphosphonates, which carry a powerful electron-releasing p-alkoxy group, yielded products resulting from phosphonate group migration from C to N or elimination (dialkyl N-arenecarbonylphosphoramidates, 13, and arenecarbonitriles, 17, respectively). These counterintuitive results are rationalized by application of the concept of "degree of electron demand" to this area of intramolecular rearrangements. The possible existence of an additional pathway for the Schmidt rearrangement, involving protonation of the iminodiazonium ion, is proposed.
- Sprecher, Milon,Kost, Daniel
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p. 1016 - 1026
(2007/10/02)
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- New N-aryl isoxazolecarboxamides and N-isoxazolylbenzamides as anticonvulsant agents
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We prepared a series of N-aryl isoxazolecarboxamide, N-isoxazolylbenzamide compounds and derivatives and studied their anticonvulsant action in MES and MMS tests. Some of these reveal considerable activity, especially with respect to MES test. The disubstitution in the 2.6-position on the phenyl ring by two methyl groups would appear to be of primary importance for the activity. The amide bridge between the phenyl and isoxazolic rings, whether of the anilide or benzamide type, seems to show similar anticonvulsant behavior. We have selected the derivatives 8 (N-(2.6-dimethylphenyl)-5-methyl-3-isoxazolecarboxamide, 12 (N-(2.6-dimethylphenyl)-5-hydroxymethyl-3-isoxazolecarboxamide) and 51 (N-(5-methyl-3-isoxazolyl)-2.6-dimethylbenzamide) which are presently being studied in more extended pharmacological tests.
- Lepage,Tombret,Cuvier,Marivain,Gillardin
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p. 581 - 593
(2007/10/02)
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- N-phenyl-N'-pyridinylureas as anticonvulsant agents
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A series of N-phenyl-N'-pyridinylureas was examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N'-(4-pyridinyl)urea series, with 37 exhibiting the best overall anticonvulsant profile. Compound 37 was effective against seizures induced by maximal electroshock but did not protect mice from clonic seizures produced by the convulsant pentylenetetrazol. The overall pharmacological profile suggests that 37 would be of therapeutic use in the treatment of generalized tonic-clonic and partial seizures. Compound 37 was selected for Phase 1 clinical trials.
- Pavia,Lobbestael,Taylor,Hershenson,Miskell
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p. 854 - 861
(2007/10/02)
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- Oxidation hair-dyeing preparations
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Oxidation hair-dyeing preparations which contain as couplers N-(2-4dihydroxbenzylidene)-amino compounds corresponding to the following formula STR1 in which A is a group corresponding to one of the following formulae STR2 or salts thereof and the developers normally present in oxidation hair dyes. p-Phenylenediamine and derivatives thereof are particularly suitable as developers. Yellow to olive-brown colors of high fastness are obtained.
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