121-41-4 alkyls. The 1,4-dihydropyridine chiral hybrid hydrogenation reagent has improved an asymmetric conversion rate, simple preparation and synthesis, can effectively reduce production costs, and is suitable for industrial production and application.
C07C 47/228 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing six-membered aromatic rings, e.g. phenylacetaldehyde
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/56 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and doubly-bound oxygen atoms bound to the carbon skeleton
C07C 47/23 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing six-membered aromatic rings, e.g. phenylacetaldehyde polycyclic
2.
3,5-DICARBOXYLIC ACID ESTER-1,4-DIHYDROPYRIDINE HYDROGENATING REAGENT, AND PREPARATION METHOD THEREFOR AND USE THEREOF
A 3,5-dicarboxylic acid ester-1,4-dihydropyridine hydrogenating reagent, and a preparation method therefor and the use thereof. The hydrogenating reagent has a structure as represented by formula (I) and has a good hydrogenation efficiency. The synthesis method is simple and the reaction conditions are mild. The production cost can be effectively reduced and the production safety can be improved.
The present invention relates to a preparation method for an aprepitant intermediate impurity. The preparation method comprises the following reaction steps: (A) carrying out a Grignard reaction on a raw material 1 and a Grignard reagent 4-fluorophenylmagnesium halide; (B) carrying out a reduction reaction on a reaction product obtained in step (A) and a reducing agent to obtain a compound 4; (C) carrying out a debenzylation reaction on the obtained compound 4 and a deprotection reagent to obtain a crude product 5; (D) reacting the obtained crude product 5 with a protective reagent in the presence of a solvent and an alkali to obtain a compound 6; and (E) carrying out a deprotection reaction on the obtained compound 6 and an acid or alkali in the presence of a solvent, and carrying out separation and purification to obtain a refined product 5. According to the method, the compound 4 is obtained by means of the reduction reaction, and then undergoes the debenzylation reaction to synthesize the compound 5, so the compound 5 can be successfully synthesized, and the yield and purity of the crude product 5 are greatly improved. Furthermore, the crude product 5 reacts with the protective reagent and is purified to obtain the compound 6, and the compound 6 is subjected to the deprotection reaction, and then is separated by means of conventional column chromatography to obtain the high-purity compound 5.
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 217/10 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical containing six-membered aromatic rings
Disclosed in the present invention is a (S)1-phenyl-1,2,3,4-tetrahydroisoquinoline synthesis method, comprising the following steps: 1) dissolving raw material 1 in a solvent, and adding an alkali and a catalyst; and 2) carrying out gas replacement by using hydrogen to form a hydrogen atmosphere, and carrying out a pressurization reaction to obtain (S)1-phenyl-1,2,3,4-tetrahydroisoquinoline 2, wherein the catalyst is a BIAMH system catalyst, a D-BIMAH system catalyst, or a P-BIMAH system catalyst.
C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
5.
NEW METAL RUTHENIUM COMPLEX HAVING NITROGEN LIGAND, PREPARATION METHOD THEREFOR, AND USES THEREOF
The present invention relates to a new metal ruthenium complex having glyphosate and nitrogen ligands, the preparation method therefor, and uses thereof. Provided is a transition metal complex of a new structure having glyphosate ligand and nitrogen ligand having a structural characteristic of NH2-N(sp2). The overall structural formula (I) of the metal ruthenium complex is: [RuLmL'ΧΥ], where X and Y can be identical or different. X can be chlorine, bromine, iodine, or hydrogen, and Y can be chlorine, bromine, iodine, or ΒH4. Also disclosed are a preparation method for and uses of the transition metal complex. The metal ruthenium complex and the nitrogen ligand mentioned in the present invention are easy to synthesize and can be used in catalytic asymmetric hydrogenation reactions, in particular in catalytic asymmetric hydrogenation reactions of ketones having aryl or unsaturated alkyl at the α position, diaryl ketone and analogues thereof, ketones having tert-alkyl at the α position, ketones having a heteroatomic group at the α position, β-Ν, Ν-dimethylamino-α-acetophenone and derivatives thereof, and other aryl-alkyl ketone compounds. When the metal ruthenium complex is used for catalytic hydrogenation of a ketone, the metal complex can be prepared in-situ.
The present invention concerns a novel transition metal complex having nitrogen-containing heterocyclic ligands and phosphine ligands, the preparation thereof and the uses thereof in asymmetric catalytic hydrogenation and hydrogen transfer. The transition metals in the complex are Ru, Rh, Ir, Pd, Pt, Co, Ni or Os, there is one nitrogen-containing heterocyclic ligand, and two monophosphine ligands or one diphosphine ligand. The complex is obtained at temperatures in the range of 0°C - 120°C through a reaction of transition metal compounds, a dinitrogen or mononitrogen ligand and a diphosphine or monophosphine ligand in an organic solvent for 0.5 to 20 hours. The complex is used for catalysed asymmetric transfer hydrogenation or asymmetric hydrogenation reactions, and is used in particular in ketones, esters, acetophenones and their derivatives where α is steric alkyl, in benzophenone and its derivatives, in β-N, N-dimethylamino-α acetophenone and its derivatives and in catalysed asymmetric hydrogenation reactions of other ketone compounds.
C07B 41/02 - Formation or introduction of functional groups containing oxygen of hydroxy or O-metal groups
C07C 29/145 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen-containing functional group of C=O containing groups, e.g. —COOH of ketones with hydrogen or hydrogen-containing gases
C07C 31/125 - Monohydroxylic acyclic alcohols containing five to twenty-two carbon atoms
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Sandoval, Christian A
Li, Yue-Hui
Abstract
The invention relates to a novel class of ruthenium complexes containing phosphine and hybrid amine ligands, their preparation and use as catalysts in the reduction of simple ketones to alcohols by molecular hydrogenation. The reactivity and enantioselectivity of such complexes in the asymmetric hydrogenation of simple ketones could be enhanced by the addition of some selective additives.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
ENANTIOTECH CORPORATION LIMITED (China)
Inventor
Sandoval, Christian A
Li, Yuehui
Abstract
The present invention relates to a ruthenium or other complex of formula as follows, and its synthesis and use thereof. The preparation method of the transition metal complex is to react the dinitrogen ligand of the structural feature of -NH2-N(sp2) with the transition metal and then to form the transition metal complex, which is composed of bidentate phosphine ligand or bidentate nitrogen ligand. The transition metal complex is useful for catalyzing hydrogenation, especially for unsymmetrical hydrogenation reaction of hypnone and its derivatives, benzophenone and its derivatives, beta-N, N-dimethy-alpha-benzol-acetone and its derivatives and other ketones.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Sandoval, Christian A
Li, Yuehui
Abstract
The invention relates to a novel class of ruthenium complexes containing phosphine and hybrid amine ligands, their preparation and use as catalysts in the reduction of simple ketones to alcohols by molecular hydrogenation. The reactivity and enantioselectivity of such complexes in the asymmetric hydrogenation of simple ketones could be enchanced by the addition of some selective additives.
B01J 31/28 - Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups of the platinum group metals, iron group metals or copper
patents
