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 amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.
Claims36
A method for coupling amino acids into peptides or peptidomimetics, the improvement comprising:
- combining an amino acid, a carbodiimide, an activator additive, and a base, with the base in an amount of less than 1 equivalent compared to the amino acid to be activated;
- and carrying out the activation and coupling at a temperature greater than 30° C.
A method for coupling carboxylic acids and amines, the improvement comprising:
- combining a carboxylic acid, an amine, a carbodiimide, an activator additive, and a base, with the base in an amount of less than 1 equivalent compared to the amine;
- and carrying out activation and coupling at a temperature greater than 30° C.
A solid phase method for coupling amino acids into peptides or peptidomimetics, the improvement comprising:
- combining a hyper-acid sensitive linker connecting a peptide and a resin, an amino acid, a carbodiimide, an activator additive, and a base, with the base is present in an amount of less than 1 equivalent compared to the amino acid to be activated;
- and carrying out the activation and coupling at a temperature greater than 30° C.
Dependencies are inferred from the claim text.