PROCESS FOR PEPTIDE SYNTHESIS USING A REDUCED AMOUNT OF DEPROTECTION AGENT

WIPO Patent Application WO2005063791

B1

The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.

GUINN MARTIN R (US)
HODGES LEWIS M (US)
JOHNSTON DAVID A (US)
MOORLAG HENDRICK (US)
SCHWINDT MARK A (US)

PCT/EP2004/014599

November 10, 2005

December 22, 2004

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HOFFMANN LA ROCHE (CH)
GUINN MARTIN R (US)
HODGES LEWIS M (US)
JOHNSTON DAVID A (US)
MOORLAG HENDRICK (US)
SCHWINDT MARK A (US)

C07K1/02; C07K1/04; (IPC1-7): C07K1/02; C07K1/04

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