Patent classifications
C07D231/26
1,2-bis(diphenylphosphinoalkylamido)-1,2-disubstituted ethane, and its synthesis and application
The present invention relates to the design and synthesis of a class of novel chiral phosphine ligand, 1,2-bis(diphenylphosphinoalkylamido)-1,2-disubstituted ethane, and use in asymmetric catalytic reactions, such as asymmetric catalytic synthesis of pyrazoline-5-one with a chiral quaternary carbon center, i.e., highly enantioselective synthesis of 3-methyl-4-benzyl-4-(2-butyl-2,3-butadienyl)pyrazoline-5-one by using 3-methyl-4-benzylpyrazoline-5-one and benzyl (2-butyl-2,3-butadienyl) carbonate with tris(dibenzylideneacetone)dipalladium-chloroform adduct and this novel ligand as catalysts. The ligand designed by this present invention has the following advantages: the structure is novel, the synthesis and enlarge are simple, the enantioselective control effect in the practical reaction is excellent, which has a broad application prospect in chiral catalysis.
Analysis method of 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient, treatment for amyotrophic lateral sclerosis, inhibition of progression of amyotrophic lateral sclerosis, and method of producing medicament containing 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient
A method of analyzing phenylhydrazine content in a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient includes obtaining a first measured value by measuring a phenylhydrazine content of a standard solution including phenylhydrazine or a salt thereof, a first acidic water and a first water-soluble organic solvent and having a phenylhydrazine concentration of 0.01 g/mL to 10 g/mL, obtaining a second measured value by measuring a phenylhydrazine content in a sample solution including a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient, a second acidic water and a second water-soluble organic solvent, and detecting a phenylhydrazine content in a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient based on the first measured value and second measured value. The first acidic water includes hydrochloric acid, the first water-soluble organic solvent is acetonitrile and/or methanol, the second acidic water includes hydrochloric acid, and the second water-soluble organic solvent is acetonitrile and/or methanol.
Analysis method of 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient, treatment for amyotrophic lateral sclerosis, inhibition of progression of amyotrophic lateral sclerosis, and method of producing medicament containing 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient
A method of analyzing phenylhydrazine content in a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient includes obtaining a first measured value by measuring a phenylhydrazine content of a standard solution including phenylhydrazine or a salt thereof, a first acidic water and a first water-soluble organic solvent and having a phenylhydrazine concentration of 0.01 g/mL to 10 g/mL, obtaining a second measured value by measuring a phenylhydrazine content in a sample solution including a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient, a second acidic water and a second water-soluble organic solvent, and detecting a phenylhydrazine content in a 3-methyl-1-phenyl-2-pyrazolin-5-one active pharmaceutical ingredient based on the first measured value and second measured value. The first acidic water includes hydrochloric acid, the first water-soluble organic solvent is acetonitrile and/or methanol, the second acidic water includes hydrochloric acid, and the second water-soluble organic solvent is acetonitrile and/or methanol.
ACSS2 inhibitors and methods of use thereof
The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and dmg resistant cancer of various types.
ACSS2 inhibitors and methods of use thereof
The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and dmg resistant cancer of various types.
ACSS2 INHIBITORS AND METHODS OF USE THEREOF
The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and dmg resistant cancer of various types.
ACSS2 INHIBITORS AND METHODS OF USE THEREOF
The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and dmg resistant cancer of various types.