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US 10,308,677 B2Granted
Coupling method for peptide synthesis at elevated temperatures
AssigneeCEM Corporation
InventorsJonathan M. Collins, Sandeep Kumar Singh
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Abstract
An improved method for coupling carboxylic acids and amines is disclosed that includes the steps of combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid, a carbodiimide, an activator additive, and a base, and carrying out the activation and coupling at a temperature greater than 30° C.
Claims18
In a method for coupling carboxylic acids and amines, the improvement comprising:
- combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid to be activated, a carbodiimide, an activator additive, and a base wherein the base is in an amount of less than 1 equivalent compared to the carboxylic acid to be activated;
- carrying out the activation of the carboxylic acid;
- and
- coupling the activated carboxylic acid to the amine connected to the resin by a hyper-acid sensitive linker at a temperature greater than 30° C.
1 more element
A mixture comprising:
- a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid to be activated, a carbodiimide, an activator additive, and a base wherein the base is in an amount of less than 1 equivalent compared to the carboxylic acid to be activated;
- and
- maintained at a temperature greater than 30° C.
Dependencies are inferred from the claim text.