Patent classifications
C07B43/04
DIVERSITY-ORIENTED SYNTHESIS OF N,N,O-TRISUBSTITUTED HYDROXYLAMINES FROM ALCOHOLS AND AMINES BY N-O BOND FORMATION
In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
NOVEL ANNULATION CATALYSTS VIA DIRECT C-H BOND AMINATION
Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. C—H bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield C—N bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.
METHOD FOR THE INDUSTRIAL PRODUCTION OF 2-HALO-4,6-DIALKOXY-1,3,5-TRIAZINES AND THEIR USE IN THE PRESENCE OF AMINES
A method for stabilization of collagen matrices and of condensation of natural and synthetic polymers that uses 2-halo-4,6-dialkoxy-1,3,5-triazines in the presence of one or more amines as activating agents for reactions of crosslinking, condensation, grafting, and curing of collagen matrices, cellu lose, modified celluloses, polysaccharides, acid unsaturated polymers, and chiral and non-chiral amines, etc. Forming an integral part of the present invention is also the method for production on an industrial scale of 2-halo-4,6-dialkoxy-1,3,5-triazines.
METHOD FOR THE INDUSTRIAL PRODUCTION OF 2-HALO-4,6-DIALKOXY-1,3,5-TRIAZINES AND THEIR USE IN THE PRESENCE OF AMINES
A method for stabilization of collagen matrices and of condensation of natural and synthetic polymers that uses 2-halo-4,6-dialkoxy-1,3,5-triazines in the presence of one or more amines as activating agents for reactions of crosslinking, condensation, grafting, and curing of collagen matrices, cellu lose, modified celluloses, polysaccharides, acid unsaturated polymers, and chiral and non-chiral amines, etc. Forming an integral part of the present invention is also the method for production on an industrial scale of 2-halo-4,6-dialkoxy-1,3,5-triazines.
Carbon-coated transition metal nanocomposite material, preparation and application thereof
A carbon-coated transition metal nanocomposite material includes carbon-coated transition metal particles having a core-shell structure. The shell layer of the core-shell structure is a graphitized carbon layer doped with oxygen and/or nitrogen, and the core of the core-shell structure is a transition metal nanoparticle. The nanocomposite material has a structure rich in mesopores, is an adsorption/catalyst material with excellent performance, can be used for catalyzing various hydrogenation reduction reactions, or used as a catalytic-oxidation catalyst useful for the treatment of volatile organic compounds in industrial exhaust gases.
Carbon-coated transition metal nanocomposite material, preparation and application thereof
A carbon-coated transition metal nanocomposite material includes carbon-coated transition metal particles having a core-shell structure. The shell layer of the core-shell structure is a graphitized carbon layer doped with oxygen and/or nitrogen, and the core of the core-shell structure is a transition metal nanoparticle. The nanocomposite material has a structure rich in mesopores, is an adsorption/catalyst material with excellent performance, can be used for catalyzing various hydrogenation reduction reactions, or used as a catalytic-oxidation catalyst useful for the treatment of volatile organic compounds in industrial exhaust gases.
Hydrogenation of nitrogen
The invention relates to methods for the hydrogenation of nitrogen by reducing a N≡N bond in a metal complex comprising a N≡N bond by reacting the metal complex with a Lewis acid, wherein the metal complex comprises Cr, Mo, W, Mn, Tc, Re, Fe, Ru, Os, Co, Rh, Ir, Ni, Pd or Pt.
Hydrogenation of nitrogen
The invention relates to methods for the hydrogenation of nitrogen by reducing a N≡N bond in a metal complex comprising a N≡N bond by reacting the metal complex with a Lewis acid, wherein the metal complex comprises Cr, Mo, W, Mn, Tc, Re, Fe, Ru, Os, Co, Rh, Ir, Ni, Pd or Pt.
Asymmetric synthesis of Azaspiro compounds
The present invention relates to an improved asymmetric synthesis of azaspiro or diazaspiro compound (hereafter referred to as the compound 5, (5.sup.A) or (5.sup.N)) or their pharmaceutically acceptable salts and derivatives; through the formation of intermediate compounds 4, (4.sup.A) or (4.sup.N) respectively. The process comprises an unusual substrate specific highly diastereoselective as well as enantio-enriched 1-substituted 2-azaspiro[3.3]heptane or 1-substituted 2-diazaspiro[3.3]heptane compounds with high diastereoselectivity by addition of a cyclobutane carboxylate anion to a Davis-Ellman's imine, followed by reduction and cyclisation resulting in the selective formation of azaspiro or diazaspiro intermediate compound 4, (4.sup.A) or (4.sup.N); which on subsequently removing the sulfinyl group provides corresponding azaspiro or diazaspiro compound 5, (5.sup.A) or (5.sup.N) respectively.
PROCESS FOR PREPARING 4-AMINO-PYRIDAZINES
Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.