Nucleophile-stable thioester generating compounds, methods...

Details Nucleophile-stable thioester generating compounds, methods... Nucleophile-stable thioester generating compounds, methods...

2005-12-20

2005-12-20

Lukton, David (Department: 1653)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Synthesis of peptides

C530S334000, C530S345000, C554S101000, C560S001000

Reexamination Certificate

active

06977292

ABSTRACT:
The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.

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