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US 2005/0239695 A1Published application
Process for the formation of disulfide bonds in cyclic peptides
AssigneeCHEMI SPA, Cinisello Balsamo
InventorsSilvana Cappelletti, Olivia Storace, Paola Annoni, Massimo Pinori
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Abstract
A non-oxidative process is described for the formation of an intramolecular disulfide bond in precursors of the peptide or peptidomimetic type; said process comprises the preparation of a linear intermediate containing an —SH group in the S-sulfonate form and a second —SH group which is obtainable in the free form by means of acid treatment.
Claims20
A process for the cyclisation of peptide or peptidomimetic molecules comprising:
- (a) preparation of a linear precursor containing an -S-sulfonate group and an —SH group protected with an acid-labile protective group;
- (b) selective liberation of the —SH group protected with said acid-labile protective group in an anhydrous aprotic non-polar organic solvent in the presence of at least one carbocation scavenger at a pH of less than 3;
- (c) dissolution and subsequent cyclisation of the partially deprotected linear precursor at a pH of between 5 and 9.
Dependencies are inferred from the claim text.