Processes for coupling amino acids using bis-(trichloromethyl) carbonate
US6512092B2 · kind B2 · utility
5Cited by
1References
14Claims
0Family size
Assignee
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Key dates
| Filing date | Jan 9, 2001 |
| Grant date | Jan 28, 2003 |
| Priority date | — |
| Expiry date | Mar 26, 2021 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A process is disclosed for using triphosgene as an efficient and effective coupling reagent during peptide synthesis, by in situ generation of amino acid chloride from a protected amino acid. This process is particularly useful for the coupling to sterically hindered amino acid residues, or for other difficult couplings. Furthermore, the same reagent can be used for the derivatization of peptides by formation of an amide bond between a free amine on a peptide and a carboxylic acid, or for the coupling of an amino acid to a solid support.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.