Efficient and scalable synthesis of nicotinoylribosides and reduced nicotinoylribosides, modified derivatives thereof, phosphorylated analogues thereof, adenyl dinucleotide conjugates thereof, and novel crystalline forms thereof

ES3078332T3Undetermined Publication Date: 2026-09-10THE QUEENS UNIVERSITY OF BELFAST (50 00) +1
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Patent Information

Application Number
ES2017870568T
Authority / Receiving Office
ES · ES
Patent Type
Patents
Current Assignee / Owner
Priority Date
2017-11-10
Filing Date
2017-11-10
Publication Date
2026-09-10
Estimated Expiration
2037-11-10

AI Technical Summary

Technical Problem

Current methods for synthesizing nicotinoyl ribosides, reduced nicotinoyl ribosides, and their derivatives face challenges such as low yields, batch-to-batch quality variation, use of corrosive and expensive reagents, and inefficiencies in solvents and reaction conditions, making them difficult to scale up for pharmaceutical and nutraceutical applications.

Method used

Development of scalable methods using liquid-assisted mixing and extrusion processes with minimal solvent use, sealed conditions, and continuous liquid-liquid extraction, along with mechanochemistry to optimize conversion and reaction times, leading to the production of novel crystalline forms of nicotinic acid ribosides and derivatives.

Benefits of technology

These methods provide atom-efficient, time- and energy-efficient, and scalable processes for producing stable crystalline forms of nicotinoyl ribosides and derivatives, enhancing their availability and suitability for pharmaceutical and nutraceutical uses.

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Abstract

This disclosure provides methods for making nicotinoyl riboside compounds or derivatives of formula (I): where X”, Z1, Z2, n, R1, R2, R3, R4, R5, R6, R7 and R8 are described herein, reduced analogues thereof, modified derivatives thereof, phosphorylated analogues thereof and adenylyl dinucleotide conjugates thereof, or salts, solvates or prodrugs thereof; and novel crystalline forms thereof.
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