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US 10,858,390 B2Granted
Use of excess carbodiimide for peptide synthesis at elevated temperatures
AssigneeCEM Corporation
InventorsJonathan M. Collins, Sandeep K. Singh
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Abstract
An improved method of coupling amino acids into peptides or peptidomimetics is disclosed in which the activation and coupling are carried out in the same vessel, in the presence of a carbodiimide in an amount greater than 1 equivalent as compared to the amino acid, in the presence of an activator additive, and at a temperature greater than 30° C.
Claims5
In a method of coupling initially Fmoc-protected amino acids into peptides or peptidomimetics, the improvement comprising:
- carrying out activation and coupling in the same vessel;
- incorporating a carbodiimide in an amount between 1.5 and 4 equivalents as compared to the amino acid to be activated, wherein the amino acid is initially Fmoc-protected;
- in the presence of an activator additive;
- and
- at a temperature greater than 70° C.
2 more elements
Dependencies are inferred from the claim text.