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Acta Poloniae Pharmaceutica - Drug Research, ISSN 0001-6837, 2018, Volume 75, Issue 3, pp. 649 - 658
A series of N-(2-oxo-2-(phenylamino) ethyl) substituted-4-carboxamide derivatives were synthesized as local anesthetic agents. The structures of carboxamide... 
Carboxamide | Surface local anesthetic activity | Infiltration local anesthetic activity | Hepatotoxicity | SET | SAFETY | hepatotoxicity | TETRACAINE | DRUG DISCOVERY | PHARMACOLOGY & PHARMACY | surface local anesthetic activity | TOXICITY | EFFICIENCY | infiltration local anesthetic activity
Journal Article
Tetrahedron, ISSN 0040-4020, 01/2017, Volume 73, Issue 4, pp. 338 - 350
In this paper, we describe a four step synthesis of 1,3-dioxo-1,3-dihydroisobenzofuran-4-carboxamides starting from (hetero)arylcarboxamides. These are first... 
(E)-N-(1-(dimethylamino)ethylidene)-carboxamides | 1,3-Dioxo-1,3-dihydroisobenzofuran-4-carboxamides | Enaminones | Aroylacetamidines | Carboxamides | CHEMISTRY, ORGANIC | (E)-N-(1-(dimethylamino)ethylidene)carboxamides | Maleic anhydride
Journal Article
Tetrahedron, ISSN 0040-4020, 2017, Volume 73, Issue 4, pp. 338 - 350
In this paper, we describe a four step synthesis of 1,3-dioxo-1,3-dihydroisobenzofuran-4-carboxamides starting from (hetero)arylcarboxamides. These are first... 
(E)-N-(1-(dimethylamino)ethylidene)-carboxamides | 1,3-Dioxo-1,3-dihydroisobenzofuran-4-carboxamides | Aroylacetamidines | Enaminones | Carboxamides
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 02/2018, Volume 26, Issue 4, pp. 845 - 854
Amining to develop pharmacological and improve aqueous solubility, we have identified series of TRPV1 antagonists bearing phenylquinoline moiety, exemplified... 
Phenylquinoline | Analgesia | TRPV1 | CHEMISTRY, MEDICINAL | PATENT LITERATURE | PHARMACOLOGY | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | RELIEF | DERIVATIVES
Journal Article
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 11/2006, Volume 281, Issue 46, pp. 34870 - 34879
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 10/2006, Volume 281, Issue 43, pp. 32207 - 32216
AMP-activated protein kinase (AMPK) is a heterotrimeric protein kinase that is crucial for cellular energy homeostasis of eukaryotic cells and organisms. Here... 
CELLS | ENERGY HOMEOSTASIS | PHOSPHORYLATION | SUBSTRATE | BIOCHEMISTRY & MOLECULAR BIOLOGY | ESCHERICHIA-COLI | UPSTREAM KINASE | CELLULAR-ENERGY | CREATINE-KINASE | SUBUNIT | BETA | Protein Kinases - metabolism | Protein-Serine-Threonine Kinases - analysis | Phosphorylation | Multienzyme Complexes - metabolism | AMP-Activated Protein Kinases | Aminoimidazole Carboxamide - pharmacology | Recombinant Proteins - isolation & purification | Ribonucleotides - pharmacology | Protein Isoforms - metabolism | Allosteric Regulation - physiology | Adenosine Triphosphate - metabolism | Protein-Serine-Threonine Kinases - metabolism | Recombinant Proteins - metabolism | Adenosine Monophosphate - metabolism | NAD - pharmacology | Protein-Serine-Threonine Kinases - genetics | Glutathione Transferase - metabolism | Multienzyme Complexes - genetics | Animals | Aminoimidazole Carboxamide - analogs & derivatives | Mice | Enzyme Activation | Multienzyme Complexes - analysis | Mutation | In Vitro Techniques | Protein Isoforms - genetics | Multienzyme Complexes | Allosteric Regulation | Protein-Serine-Threonine Kinases | Biochemistry, Molecular Biology | Adenosine Triphosphate | Recombinant Proteins | Adenosine Monophosphate | NAD | Life Sciences | Aminoimidazole Carboxamide | Ribonucleotides | Protein Kinases | Protein Isoforms | Glutathione Transferase
Journal Article
Organic Letters, ISSN 1523-7060, 04/2017, Volume 19, Issue 7, pp. 1614 - 1617
Nonplanar, electronically destabilized amides have emerged as powerful intermediates in organic synthesis. We report a highly selective method for... 
CATALYZED DECARBONYLATIVE BORYLATION | PRIMARY CARBOXAMIDES | FUNCTIONALIZATION | ACYLSACCHARINS | ACTIVATION | KETONE SYNTHESIS | NICKEL CATALYSIS | NITROGEN BOND-CLEAVAGE | TWISTED AMIDES | ESTERS | CHEMISTRY, ORGANIC
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 03/2014, Volume 136, Issue 9, pp. 3354 - 3357
A Cu(OAc)2-mediated C–H amidation and amination of arenes and heteroarenes has been developed using a readily removable directing group. A wide range of... 
CUPRIC ACETATE | PALLADIUM | CROSS-COUPLING REACTIONS | ACTIVATION | AROMATIC CARBOXAMIDES | ARYL | CARBON-HYDROGEN BONDS | INHIBITORS | CHEMISTRY, MULTIDISCIPLINARY | ARYLBORONIC ACIDS | CATALYZED ARYLATION | Copper | Influence
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 10/2014, Volume 136, Issue 41, pp. 14349 - 14352
We report here that an iron-catalyzed directed C–H functionalization reaction allows the coupling of a variety of aromatic, heteroaromatic, and olefinic... 
BORONIC ACIDS | ACTIVATION | ALKYL | IMINES | ARYL | CARBOXAMIDES | ORTHO-ARYLATION | CHEMISTRY, MULTIDISCIPLINARY | C-H BONDS | ALKENYLATION | METATHESIS
Journal Article
Organic Letters, ISSN 1523-7060, 11/2016, Volume 18, Issue 22, pp. 5872 - 5875
A general Negishi acylation of primary amides enabled by a combination of site-selective N,N-di-Boc activation and nickel catalysis is reported for the first... 
PRIMARY CARBOXAMIDES | ORGANOZINC REAGENTS | ACYLATING AGENTS | ORGANOMETALLIC REAGENTS | CONVERSION | NITROGEN BOND-CLEAVAGE | TWISTED AMIDES | CHEMISTRY, ORGANIC | TRANSAMIDATION | ANHYDRIDES | INHIBITORS
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 1900, Volume 137, Issue 24, pp. 7660 - 7663
Conversion of a C­(sp2)–H or C­(sp3)–H bond to the corresponding C–Me bond can be achieved by using AlMe3 or its air-stable diamine complex in the presence of... 
ORGANIC-SYNTHESIS | CROSS-COUPLING REACTIONS | AROMATIC CARBOXAMIDES | DRUG DISCOVERY | UNACTIVATED C(SP)-H | CARBON-HYDROGEN BONDS | CHEMISTRY, MULTIDISCIPLINARY | C-H BONDS | GRIGNARD-REAGENTS | PALLADIUM ACETATE | ALKYL-HALIDES
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 06/2018, Volume 140, Issue 22, pp. 6789 - 6792
Amides are an important class of organic compounds, which have widespread industrial applications. Transamidation of amides is a convenient method to generate... 
PRIMARY CARBOXAMIDES | HALIDES | ACID | SECONDARY AMIDES | AMINES | DERIVATIVES | CHEMISTRY, MULTIDISCIPLINARY | CATALYZED TRANSAMIDATION | DIRECT AMIDATION | UREAS
Journal Article
Organic Letters, ISSN 1523-7060, 02/2017, Volume 19, Issue 3, pp. 596 - 599
Co­(II)-catalyzed C–H C2 selective arylation of indoles with boronic acids through monodentate chelation assistance has been achieved for the first time. The... 
ARYL BROMIDES | FUNCTIONALIZATIONS | ANNULATION | COBALT CATALYSIS | CHLORIDES | CHEMISTRY, ORGANIC | SELECTIVE ARYLATION | BOND ACTIVATION | CARBOXAMIDES | (HETERO)ARENES | CATALYZED DIRECT ARYLATION
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 11/2013, Volume 2013, Issue 33, pp. 7453 - 7465
The synthesis of amides is of huge importance in a wide variety of industrial and academic fields and is of particular significance in the synthesis of... 
Amides | Transamidation | Amines | Carboxylic acids | Amidation | HIGHLY EFFICIENT CATALYST | REAGENT | CHEMISTRY, ORGANIC | BOND FORMATION | BORIC-ACID | CARBOXAMIDES | MEDICINAL CHEMISTRY | CONDENSATION | FORMING REACTIONS | CHLORIDE | Organic acids
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 05/2017, Volume 27, Issue 9, pp. 1989 - 1992
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 12/2015, Volume 56, Issue 49, pp. 6904 - 6907
The stable iminolactone was obtained by NBS induced bromocyclization of carboxamide . Under treatment of with DBU a tandem recyclization transformation... 
Halocyclization | Carboxamides | Corey epoxylactone | Epoxyiminolactone | CHEMISTRY, ORGANIC
Journal Article
Chemistry Letters, ISSN 0366-7022, 4/2015, Volume 44, Issue 4, pp. 410 - 421
This review focuses on chelation-assisted regioselective C–H activation with C–C or/and C–N bond formation using nickel(0) or -(II) as the catalysts, where... 
Catalytic C-H Activation | BIDENTATE-CHELATION ASSISTANCE | OXIDATIVE CYCLOADDITION | UNACTIVATED C(SP)-H BONDS | PYRIDINE-N-OXIDES | AROMATIC AMIDES | DIARYLIODONIUM SALTS | OLEFINIC CARBOXAMIDES | CHEMISTRY, MULTIDISCIPLINARY | CATALYZED DIRECT ARYLATION | ALKYL-HALIDES | C(SP)-H AMIDATION
Journal Article
Organic Letters, ISSN 1523-7060, 04/2017, Volume 19, Issue 8, pp. 2158 - 2161
The first general method is reported for transamidation of secondary carboxamides catalyzed by Pd-NHC (NHC = N-heterocyclic carbene) complexes. Commercially... 
PRIMARY CARBOXAMIDES | C CLEAVAGE | EFFICIENT CATALYST | KETONE SYNTHESIS | CATALYTIC TRANSAMIDATION | TWISTED AMIDES | NITROGEN | CHEMISTRY, ORGANIC | BOND-CLEAVAGE | SUZUKI-MIYAURA | ARYL CHLORIDES
Journal Article
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