Process for the Preparation of Phosphate-Bridged Nucleoside Conjugates

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The patent describes a new method for producing phosphate-bridged nucleoside conjugates, including nucleoside diphosphate sugars, polyphosphorylated nucleosides, dinucleoside polyphosphates, nucleoside phosphonates, and nucleotide-sugar conjugates. The process involves dissolving a nucleophile in a non-aqueous solvent and drying it, then adding a cyclosaligenyl phosphate compound to the solution. This method improves the synthesis of these important biological molecules by offering a simpler, faster, and higher-yielding pathway than existing techniques.

Use CasesContent extracted from patent full text and abstract with AI.

• Synthesis of nucleotide-sugar conjugates for research in glycobiology and metabolic engineering.
• Production of nucleoside analogs for pharmaceutical development, including antiviral and anticancer drugs.
• Creation of dinucleoside polyphosphates for studying signaling and regulatory molecules in biological systems.
• Manufacture of nucleotide triphosphates (e.g., ATP, dNTPs) for enzymatic reactions in molecular biology such as PCR and DNA sequencing.
• Preparation of nucleoside phosphonates for use as therapeutic agents (e.g., in antiviral treatments for HIV or hepatitis).

BenefitsContent extracted from patent full text and abstract with AI.

• Provides higher yields (up to 90%) compared to conventional synthesis methods, making it more efficient.
• Applicable to a wide range of substrates, including natural and modified nucleosides, sugars, phosphates, and lipids.
• Simplifies and speeds up the synthetic process; does not require extensive purification or specialized enzymes.
• Reduces issues with product isolation and hydrolytic instability common in existing methods.
• Enables the preparation of chemically stable nucleotide analogs and bioconjugates that are valuable in research and medicine.

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Patent Abstract

The invention relates to a method for producing phosphate-bridged nucleoside conjugates. According to the method, a nucleophile is first dissolved in a non-aqueous solvent and dried, and a cyclosaligenyl phosphate compound is subsequently added to the solution.