Patent classifications
C07C211/35
CYCLOPROPYLAMINES AS LSD1 INHIBITORS
This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
CYCLOPROPYLAMINES AS LSD1 INHIBITORS
This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.
Method for Efficiently Synthesizing Primary Amines
Disclosed is a method for efficiently synthesizing primary amines, which comprises using carbonyl compounds or alcohol compounds as reaction substrate, liquid ammonia or alcohol solutions of ammonia as nitrogen source, and hydrogen as hydrogen source, and reacting in reaction medium catalyzed by a cobalt-based catalyst to obtain the primary amines. Due to high catalytic activity, the method can realize the reductive amination of carbonyl compounds and the hydrogen-borrowing amination of alcohol compounds at low temperatures in a short time to obtain the primary amines with high yield, and is applicable to a wide range of substrates. The obtained primary amines can be used as raw materials with high extra value for producing polymers, medicines, dyes and surfactants. Further, the cobalt-based catalyst has a good industrial application prospect because it is magnetic which can facilitate separation and recycling of the catalyst. Moreover, the inexpensive cobalt-based catalyst can significantly reduce industrialization cost.
Method for Efficiently Synthesizing Primary Amines
Disclosed is a method for efficiently synthesizing primary amines, which comprises using carbonyl compounds or alcohol compounds as reaction substrate, liquid ammonia or alcohol solutions of ammonia as nitrogen source, and hydrogen as hydrogen source, and reacting in reaction medium catalyzed by a cobalt-based catalyst to obtain the primary amines. Due to high catalytic activity, the method can realize the reductive amination of carbonyl compounds and the hydrogen-borrowing amination of alcohol compounds at low temperatures in a short time to obtain the primary amines with high yield, and is applicable to a wide range of substrates. The obtained primary amines can be used as raw materials with high extra value for producing polymers, medicines, dyes and surfactants. Further, the cobalt-based catalyst has a good industrial application prospect because it is magnetic which can facilitate separation and recycling of the catalyst. Moreover, the inexpensive cobalt-based catalyst can significantly reduce industrialization cost.
METHODS FOR EXTRACTION, PROCESSING, AND PURIFICATION OF A SELECTED FAMILY OF TARGET COMPOUNDS FROM CANNABIS
Disclosed are methods for separating, recovering, and purifying cannabidiolic acid (CBDA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in C5-C7 hydrocarbon solvents, adding thereto a selected amine to thereby precipitate a CBDA-amine salt therefrom, dissolving the recovered CBDA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified CBDA-amine salt therefrom. The recrystallized CBDA-amine salt may be decarboxylated to form a mixture of cannabidiol (CBD) and amine. The CBD amine mixture may be acidified to separate the amine from CBD. Also disclosed are CBDA-amine salts produced with certain amines selected from groups of secondary amines, tertiary amines, diamines, amino alcohols, amino ethers, and highly basic amines.
EFFICIENT PREPARATION OF DOLASTATIN AND AURISTATIN ANALOGS THROUGH A COMMON INTERMEDIATE
Methods for making a dolastatin, auristatin or related compounds comprising the steps of providing a universal dolastatin core of Formula (I) reacting the C-terminal carboxylic acid group with an amine (A) to form an amide bond and reacting the N-terminal amine with a carboxylic acid (CA) to form an amide bond, wherein the steps can be performed in either order. Also provided are an isolated salt of the universal dolastatin core for use in preparation of dolastatins, auristatins and related compounds. Also provided are a number of intermediates and process steps which are useful for the preparation of high purity dolastatin core and high purity dolastatin and auristatin compounds.
MATERIALS COMPRISING CARBON-EMBEDDED COBALT NANOPARTICLES, PROCESSES FOR THEIR MANUFACTURE, AND USE AS HETEROGENEOUS CATALYSTS
The present invention relates to catalytically active material, comprising grains of non-graphitizing carbon with cobalt nanoparticles dispersed therein, wherein d.sub.p, the average diameter of cobalt nanoparticles in the non-graphitizing carbon grains, is in the range of 1 nm to 20 nm, D, the average distance between cobalt nanoparticles in the non-graphitizing carbon grains, is in the range of 2 nm to 150 nm, and ω, the combined total mass fraction of metal in the non-graphitizing carbon grains, is in the range of 30 wt % to 70 wt % of the total mass of the non-graphitizing carbon grains, and wherein d.sub.p, D and ω conform to the following relation: 4.5 d.sub.p/ω>D≥0.25 d.sub.p/ω. The present invention, further, relates to a process for the manufacture of material according to the invention, as well as its use as a catalyst.
MATERIALS COMPRISING CARBON-EMBEDDED COBALT NANOPARTICLES, PROCESSES FOR THEIR MANUFACTURE, AND USE AS HETEROGENEOUS CATALYSTS
The present invention relates to catalytically active material, comprising grains of non-graphitizing carbon with cobalt nanoparticles dispersed therein, wherein d.sub.p, the average diameter of cobalt nanoparticles in the non-graphitizing carbon grains, is in the range of 1 nm to 20 nm, D, the average distance between cobalt nanoparticles in the non-graphitizing carbon grains, is in the range of 2 nm to 150 nm, and ω, the combined total mass fraction of metal in the non-graphitizing carbon grains, is in the range of 30 wt % to 70 wt % of the total mass of the non-graphitizing carbon grains, and wherein d.sub.p, D and ω conform to the following relation: 4.5 d.sub.p/ω>D≥0.25 d.sub.p/ω. The present invention, further, relates to a process for the manufacture of material according to the invention, as well as its use as a catalyst.
OXIDE-SUPPORTED COBALT CATALYST CAPABLE OF ACCELERATING REDUCTIVE AMINATION
In order to enable a reductive amination reaction at a low temperature and a low hydrogen pressure, provided is a catalyst comprising cobalt supported on an oxide, the catalyst produced by a method comprising the following steps (1) to (4): (1) a step of mixing a salt containing a cobalt ion and an oxide in water, (2) a step of distilling water away from a mixed solution obtained in step (1) and drying a resulting solid material, (3) a step of calcining a dried material obtained in step (2) in a nitrogen stream, and (4) a step of reducing a calcined product obtained in step (3) in a hydrogen stream.