Patent classifications
C07H1/04
NOVEL NICOTINAMIDE DI-NUCLEOTIDE DERIVATIVES AND USE THEREOF
A compound of formula I or pharmaceutically acceptable salts and/or solvates thereof:
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Also, compositions including at least one compound of formula I, such a pharmaceutical composition, a food composition, and a cosmetic composition. Further, a method for preparing compounds of formula I and their use as therapeutic compounds for use in the treatment of pain, antineoplastic-induced cardiotoxicity or sickle cell disease.
METHODS FOR PREPARING BISPHOSPHOCINS
Methods for synthesizing Bisphosphocins use chemical modification of dialcoholic compounds avoiding the use of tetrazole and tertiary butyl hydroperoxide.
Method for preparing 3′-o-amino-2′-deoxyribonucleoside-5′-triphosphates
Methods for preparing 3′-O-amino-2′-deoxyribonucleoside-5′-triphosphates with reduced 3′-hydroxy-2′-deoxyribonucleoside-5′-triphosphate contamination by converting 3′-(N-acetone-oxime)-2′-deoxynucleoside triphosphate to 3′-O-amine-2′-deoxynucleoside triphosphate by treatment with an aryl-oxyamine and compositions produced therefrom.
Method for preparing 3′-o-amino-2′-deoxyribonucleoside-5′-triphosphates
Methods for preparing 3′-O-amino-2′-deoxyribonucleoside-5′-triphosphates with reduced 3′-hydroxy-2′-deoxyribonucleoside-5′-triphosphate contamination by converting 3′-(N-acetone-oxime)-2′-deoxynucleoside triphosphate to 3′-O-amine-2′-deoxynucleoside triphosphate by treatment with an aryl-oxyamine and compositions produced therefrom.
METHODS FOR THE PREPARATION OF DIASTEREOMERICALLY PURE PHOSPHORAMIDATE PRODRUGS
Methods for the preparation of diastereomerically pure phosphoramidate prodrugs of nucleosides, and intermediates useful for the preparation are provided. The nucleosides are useful for the treatment of hepatitis C and cancer.
METHOD FOR PREPARING CANGRELOR TETRASODIUM SALT
The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.
METHOD FOR PREPARING CANGRELOR TETRASODIUM SALT
The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.
SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE
The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE
The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
SYNTHESIS OF AN ANTIVIRAL AZASUGAR TRIPHOSPHATE
Provided are methods of making the active 5′-triphosphate form of galidesivir (compound 1) and the active 5′-triphosphate form of azasugar nucleoside analogues (compound 2):
##STR00001##
##STR00002##
a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively:
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