Patent classifications
C07C233/22
Biaryl compositions and methods for modulating a kinase cascade
The application relates to biaryl compounds, pharmaceutical compositions comprising the compounds, and methods of use the compounds for treating cell proliferation disorders.
Therapeutic compounds and methods
The invention relates to compounds of Formula (I) and methods for their preparation. Also described are pharmaceutical compositions comprising a compound of Formula (I) and their use in the treatment or prevention of conditions associated with mitochondrial dysfunction. Formula (I) ##STR00001##
Process for preparing intermediate of anti-tumor drug niraparib and intermediate thereof
Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value. ##STR00001##
Process for preparing intermediate of anti-tumor drug niraparib and intermediate thereof
Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value. ##STR00001##
DERIVATIVES OF SOBETIROME
Compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. Such compounds have the structure of Formula (I) as shown herein, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof.
DERIVATIVES OF SOBETIROME
Compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. Such compounds have the structure of Formula (I) as shown herein, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof.
PROCESS FOR PREPARING INTERMEDIATE OF ANTI-TUMOR DRUG NIRAPARIB AND INTERMEDIATE THEREOF
Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.
##STR00001##
PROCESS FOR PREPARING INTERMEDIATE OF ANTI-TUMOR DRUG NIRAPARIB AND INTERMEDIATE THEREOF
Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.
##STR00001##
Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide
Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.
Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide
Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.