Method for the Solid-Phase Based Synthesis of Phosphate-Bridged Nucleoside Conjugates

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes a method for synthesizing phosphate-bridged nucleoside conjugates—complex molecules where nucleosides are connected through phosphate groups—using a solid-phase approach. The process involves anchoring a nucleoside derivative onto a solid support, reacting it with a special cyclosaligenyl reagent, and then introducing a nucleophile to yield the desired conjugate. The method allows for efficient and high-purity production of various bioconjugates, such as oligonucleotides and nucleotide derivatives.

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

• Synthesis of DNA and RNA oligonucleotides for genetic testing, research, and diagnostics.
• Production of nucleotide analogs for use as pharmaceutical agents or enzyme inhibitors.
• Creation of labeled or chemically modified nucleosides for molecular probes or sequencing tools.
• Preparation of bioconjugates for drug delivery systems or targeted therapeutics.
• Generation of specialized nucleotide compounds for biochemical and metabolic studies.

BenefitsContent extracted from patent full text and abstract with AI.

• Enables precise and efficient assembly of complex nucleoside conjugates.
• Offers high yields and purity compared to solution-phase methods.
• Improves control over sequence and structure, allowing for customization.
• Compatible with automation, making it suitable for high-throughput and large-scale synthesis.
• Broadly applicable to a wide variety of nucleoside, nucleotide, and bioconjugate structures.
• Reduces side reactions and simplifies downstream purification steps.

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Inventors & Applicants

Patent Abstract

The invention relates to a method for producing phosphate-bridged nucleoside conjugates, in particular poly- or oligonucleosides. In the method, an immobilized cyclosaligenyl derivative of a nucleoside, nucleotide, poly- or oligonucleotide, poly- or oligonucleoside, or an analog thereof, is synthesized, and the subsequent reaction with a nucleophile yields the desired phosphate-bridged nucleoside conjugate, which may subsequently be released from the solid phase.