Processes for coupling amino acids using bis-(trichloromethyl) carbonate
US7045592B2 · kind B2 · utility
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5Claims
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Key dates
| Filing date | Dec 18, 2002 |
| Grant date | May 16, 2006 |
| Priority date | — |
| Expiry date | Dec 28, 2023 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A process is disclosed for using bis-(trichloromethyl)carbonate (triphosgene), diphosgene or phosgene as efficient and effective coupling reagents during coupling of carbohydrates to peptide chains. This process is particularly useful for the coupling to sterically hindered amino acid residues, or for other difficult couplings. The reagents can be used for the derivatization of peptides by formation of a bond between a free amine on a peptide and a carbohydrate.
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