Method for cleavage of solid phase-bound peptides from the solid phase
AssigneeSanofi-Aventis Deutschland GmbH
InventorsWolfgang Fiedler, Norbert Pleuss, Bernd Henkel, Manfred Gerken
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Abstract
The invention relates to a method for the cleavage of a solid phase-bound polypeptide from the solid phase, the method comprising contacting the solid phase, to which the polypeptide is bound, with a composition consisting essentially of trifluoroacetic acid and 1,2-ethanedithiol, at a temperature in the range of about 23° C. to about 29° C.
Claims15
A method for cleavage of a solid phase-bound polypeptide from a solid phase, the method comprising contacting the solid phase to which the polypeptide is bound, with a composition consisting essentially of trifluoroacetic acid and 1,2-ethanedithiol,
- wherein percentages of the trifluoroacetic acid and the 1,2-ethanedithiol in the composition are 100% together, including impurities, which may be present in the trifluoroacetic acid and 1,2-ethanedithiol,
- wherein a reaction is at a temperature of 25° C. to 27° C., and
- wherein the polypeptide is selected from GLP-1, analogs and derivatives thereof, exendin-3, analogs and derivatives thereof, and exendin-4, analogs and derivatives thereof.
A method for the solid-phase synthesis of a polypeptide comprising a pre-determined amino acid sequence, said method comprising:
- (a) coupling an amino acid building block comprising an unprotected C-terminal carboxyl group and a protected N-terminal amino group, C-terminally to a solid phase,
- (b) de-protecting the N-terminal amino group of the amino acid building block,
- (c) coupling an amino acid building block, comprising an unprotected C-terminal carboxyl group and a protected N-terminal amino group, C-terminally to the unprotected N-terminal amino of step (b),
- (d) optionally repeating steps (b) and (c), and
- (e) cleaving the polypeptide from the solid phase by contacting the solid phase to which the polypeptide is bound with a composition consisting essentially of trifluoroacetic acid and 1,2-ethanedithiol at a temperature of 25° C. to 27° C.,
- wherein percentages of the trifluoroacetic acid and the 1,2-ethanedithiol in the composition are 100% together, including impurities which may be present in the trifluoroacetic acid and 1,2-ethanedithiol, and
- wherein the polypeptide is selected from GLP-1, analogs and derivatives thereof, exendin-3, analogs and derivatives thereof, and exendin-4, analogs and derivatives thereof.
A method for cleavage of a solid phase-bound polypeptide from a solid phase, the method comprising contacting the solid phase to which the polypeptide is bound, with a composition consisting essentially of trifluoroacetic acid in an amount of 97% v/v and 1,2-ethanedithiol in an amount of 3% v/v,
- wherein percentages of the trifluoroacetic acid and the 1,2-ethanedithiol in the composition are 100% together, including impurities which may be present in the trifluoroacetic acid and 1,2-ethanedithiol,
- wherein a reaction temperature is above room temperature, and
- wherein the polypeptide is selected from GLP-1, analogs and derivatives thereof, exendin-3, analogs and derivatives thereof, and exendin-4, analogs and derivatives thereof.
Dependencies are inferred from the claim text.