C07H1/04

SYNTHESIS OF AN ANTIVIRAL AZASUGAR TRIPHOSPHATE
20230303611 · 2023-09-28 ·

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):

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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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CAPPING COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF

The present disclosure includes, among other things, non-natural nucleotides useful as 5′ caps for RNA nucleotides. The present disclosure also includes, among other things, compositions and methods using delivery and vaccine RNA nucleotide compositions that include non-natural nucleotides as 5′ caps.

CAPPING COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF

The present disclosure includes, among other things, non-natural nucleotides useful as 5′ caps for RNA nucleotides. The present disclosure also includes, among other things, compositions and methods using delivery and vaccine RNA nucleotide compositions that include non-natural nucleotides as 5′ caps.

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.

3″,5″-dimethoxybenzoyl-3′-amino-3′-deoxy adenosine-5′-triphosphates and pharmaceutical uses thereof

Provided are compounds compound according to Formula (I), or a pharmaceutically acceptable salt, solvate, coordination complex or prodrug thereof: wherein, R.sup.1 and R.sup.2 are independently selected from (C.sub.1-C.sub.6) alkyl. The compounds have P2X3 receptor or P2X2/3 receptor antagonist activity and are useful for the treatment of diseases and disorders characterized by activation of those receptors. ##STR00001##

3″,5″-dimethoxybenzoyl-3′-amino-3′-deoxy adenosine-5′-triphosphates and pharmaceutical uses thereof

Provided are compounds compound according to Formula (I), or a pharmaceutically acceptable salt, solvate, coordination complex or prodrug thereof: wherein, R.sup.1 and R.sup.2 are independently selected from (C.sub.1-C.sub.6) alkyl. The compounds have P2X3 receptor or P2X2/3 receptor antagonist activity and are useful for the treatment of diseases and disorders characterized by activation of those receptors. ##STR00001##

Efficient method for the preparation of Cangrelor

Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV): ##STR00001## The process is characterized by the high yield and purity of the product, and can be used industrially.

Efficient method for the preparation of Cangrelor

Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV): ##STR00001## The process is characterized by the high yield and purity of the product, and can be used industrially.

METHOD FOR PREPARING 3'-O-AMINO-2'-DEOXYRIBONUCLEOSIDE-5'-TRIPHOSPHATES
20210300961 · 2021-09-30 · ·

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.