Superior Liquid Uptake Resins for Polymer-supported Synthesis (SLURPS)

Background
Solid phase synthesis, or polymer-supported synthesis, is a technique for chemical transformations in which molecules are bound to a solid, such as a polymer bead, during the reaction and hence are easier to separate afterwards. The main benefit lies in the fact that these supports, by being insoluble, allow the easy separation of bound product from soluble reagents and contaminants. When used to support catalysts (including enzymes), they provide a means of recovering and recycling of the usually expensive catalyst. A truly universal support would be:
• compatible with all types of organic and aqueous solvents
• compatible with biomolecules (it would not interact, inhibit or promote their degradation)
• inert under chemical and enzymatic reactions conditions
• available at any desired loading level (tunability) and with very high loading levels (cost and process advantage)
• available with a wide range of functional groups so that any desired linker, spacer, or any other molecule of interest can be integrated
• mechanically robust in a flow reactor format and allow for high control of flow properties via specific variations in cross-linking levels and co-monomer incorporation

To date, no single support exhibits all of these desired characteristics.

Invention
This invention concerns a newly developed polymer support composed of 1,4-butanediol vinyl ether derivatives cross-linked with 1,4-butanediol divinyl ether. Swelling studies of these materials show enhanced solvent compatibility as compared to existing high-loading resins and successful organic and peptide synthesis has already been carried out using these supports with outstanding results. The performance is better compared to most and at least as good as the best currently used supports for synthesis. Furthermore polyethers have been shown to be compatible with biomolecules and not subjected to enzymatic degradation. Therefore, unlike most supports for synthesis, SLURPS allow for biotechnology applications.

Benefits
SLURPS are the closest to a truly universal polymer support, exhibiting the following characteristics:
• Excellent performance as support for synthetic transformations as well as polypeptide synthesis
• Excellent control of loading levels and high maximum loading levels (≥ 8.5 mmol/g)
• Good swelling properties and therefore solvent compatibility across the whole solvent polarity scale from hexane to acetone to water
• Excellent chemical stability
• Ease of synthesis including control of comonomer incorporation and levels of crosslinking via a living polymerisation process
• A wide range of functional groups easily accessible
• Fast swelling rates and ease of handling (filtration)
• Mechanically robust
• FTIR transparent allowing on-support monitoring of reactions
• 2nd generation SLURPS can be synthesised from commercially available monomers offering the potential of further performance enhancement to cover an even wider range of end-user properties

IP & Commercial Opportunity A patent has been granted (WO03/104294). The supports have been tested in a number of different laboratory syntheses. We are now seeking to contact partners who would be interested in licensing the technology for commercial applications.

Type of Offer: Licensing



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