On-resin peptide cyclization

Details On-resin peptide cyclization On-resin peptide cyclization

C - Chemistry, Metallurgy

07

K

C07K 1/04 (2006.01) C07K 1/06 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2588098

Method of peptide synthesis, comprising the steps of a. synthesizing a peptide linked to a solid phase which peptide comprises at least one cysteine, homo- or nor-cysteine residue, which cysteine is protected in its side chain by a S- tert.butyl-sulphenyl group b. either coupling N-terminally a further amino acid having a 3,3'-dithio-(1-~carboxy-propyl)-propionyl-radical on its N.alpha. or deprotecting the N.alpha. of the N-terminal amino acid and reacting the free N.alpha. with 3,3'-dithio-propionic acid imide to yield the corresponding N.alpha.-3,3'-dithio-(1-carboxy-propyl)-~propionamide or deprotecting the N.alpha. of the N-terminal amino acid and reacting the free N.alpha. with a compound of formula IV R7-S-S-[CH2]2-COOH IV wherein R7 is aryl-, including heteronuclear aryl, or is aralkyl-, alkylaryl- or alkyl-, which may be further substituted with halogeno, amido, ester, carboxy or ether, and c. reacting the peptide with a S-tert.Butyl-sulphenyl-protection group removing reagent, and d. cyclizing the peptide by means of disulfide bond formation, preferably cyclizing the peptide in the presence of air and/or oxygen.

Nouveau composé représenté par la formule (I).

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