405results about "Amino group formation/introduction" patented technology

The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.

The invention discloses a nitrogen-doped carbon material supporting cobalt catalyst and a method therewith of catalytic hydrogenation reductive amination to produce primary amine compounds. The catalyst is prepared through the steps of: 1) preparing a MOF material ZIF-67; and 2) under protection of nitrogen gas, calcining the MOF material ZIF-67 at 200-1000 DEG C for 1-10 h to produce the nitrogen-doped carbon material supporting cobalt catalyst Co / N-C. The method of catalytic hydrogenation reductive amination to produce the primary amine compounds with the catalyst includes the steps of: in an organic solvent, adding a carbonyl compound, ammonia water and the nitrogen-doped carbon material supporting cobalt catalyst, feeding hydrogen gas, and performing a reaction at 50-150 DEG C under 0.1-5 MPa for 0.5-20.0 h to produce the amine compounds. The preparation method of the catalyst is simple in operations. The catalyst can be used for producing the primary amine compounds in a manner of catalytic hydrogenation reductive amination. In the method, the primary amine compounds are produced with the carbonyl compound as a raw material through catalytic hydrogenation by means of the catalyst, so that the method has mild reaction conditions and is high in yield.

The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and / or prodrugs thereof.

The present invention discloses an ion liquid cross-linked polymer supported nanometer palladium metal catalytic material, which is short for P(DVB-DIIL)-Pd, and has the structure defined in the specification. The invention further discloses a preparation method of the catalytic material, and applications of the catalytic material in preparation of aromatic amine compounds through liquid phase catalytic hydrogenation of nitro aromatic hydrocarbons. According to the present invention, the ion liquid cross-linked polymer supported nanometer palladium metal catalytic material can provide high catalytic selectivity and high conversion rate for the liquid phase hydrogenation reactions of a variety of nitro aromatic hydrocarbon compounds, and can be recycled.

This invention provides a process for conducting Stille coupling reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in Stille couplings of aryl halides. A Stille coupling can be carried out by mixing, in a liquid medium, at least one strong base; at least one aryl halide or aryl pseudohalide in which all substituents are other than stannyl groups, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one halogen atom selected from the group consisting of a chlorine atom, a bromine atom, and an iodine atom; at least one organotin compound wherein the tin atom is quaternary, wherein one group bound to the tin atom is unsaturated at the alpha or beta position, and wherein each of the remaining groups bound to the tin atom is a saturated group; at least one metal compound comprising at least one metal atom selected from nickel, palladium, and platinum, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene. One preferred type of N-heterocyclic carbene is an imidazoline-2-ylidene of the formulawherein R1 and R2 are each, independently, alkyl or aryl groups having at least 3 carbon atoms, R3 and R4 are each, independently, a hydrogen atom, a halogen atom, or a hydrocarbyl group.

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

The invention discloses a preparation method for palbociclib (I). The preparation method comprises the following steps: performing cyclization reaction on 2-acetyl-2-butenoic acid methyl ester and malononitrile under an alkaline condition to generate 1,4,5,6-4H-2-methoxyl-4-methyl-5-acetyl-6-oxo-3-pyridine carbonitrile (II); performing substitution reaction on the intermediate (II) and cyclopentane halide (III) under the action of an acid-binding agent to generate N-cyclopentyl-1,4,5,6-4H-2-methoxyl-4-methyl-5-acetyl-6-oxo-3-pyridine carbonitrile (IV); performing condensation reaction on the intermediate (IV) and N-[5-(1-piperazinyl)-2-piperidyl]carbamidine (V)to generate 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]-5,6-dihydropyrido[2,3-d]pyrimidine-7(8H)-ketone (VI); performing dehydrogenation reaction on the intermediate (VI) and sodium selenate to generate the palbociclib (I). The preparation method for the palbociclib has the advantages that the raw material is easy to obtain, the process is simple, high efficiency and environmental protection are achieved, and the preparation method is suitable for industrial production.

The invention relates to a process for carrying out asymmetrical hydroxylamine amination reaction and dual hydroxide reaction, wherein synthesized high polymer tethered Cinchonideine alkaloid ligand is utilized for raising yield and selectivity for the reaction product, the catalyst can be used repeatedly. The process is especially suitable for the mass production of Taxol synthesis and its C13 side chains, the used synthesized high polymer tethered Cinchonideine alkaloid ligand has the structural formula as disclosed in the specification, wherein PEG is polyoxyethylene glycols, R=H or OCH3.

A process for the hydrogenation, using molecular hydrogen (H2) of a catalytic system, wherein the catalytic system includes a base and a complex of formula (II):Ru(P2N2)Y2  (II)wherein Y represent simultaneously or independently a hydrogen or halogen atom, a hydroxy group, or an alkoxy, carboxyl or other anionic radical, and P2N2 is a tetradentate diimino-diphosphine ligand.

The invention provides a method for preparing aromatic primary amine by taking ammonia water as an ammonia source in a water phase system. In the method, aromatic halogenate and the ammonia water are used as raw materials, water is used as a solvent, at room temperature or under the heating condition of common oil bath, carbonates, fluorides, phosphates and hydroxides of alkali metals or alkaline-earth metals are taken as alkalis, and a catalytic reaction is preformed through adding a surfactant and using a temary catalysis system composed of copper catalyst, hydrazide and ketone. The method has the characteristics that the operation is simple, wide substrate application range is wide, the product is simple and easy to separate, the yield is high, the process is economic and is environment-friendly and the like; and reaction conditions are flexible, thus corresponding room temperature or heating mode can be selected according to practical requirements. In addition, the environment friendliness of the reaction is effectively improved by using water as a reaction solvent, thereby better conforming to the development requirements of green chemistry. Especially, the substrate is wide in application range and has wide application prospects in the aspects of preparing natural products, medicines and pesticides.