METHOD OF REMOVING PROTECTING GROUP FROM PROTECTED PEPTIDE

摘要

PURPOSE:Methanesulfonic acid or its substituted analog and a specific thioether derivative are used as reagent for removing protecting groups on peptide, thus removing the protecting groups with one stage without side reaction and producing physiologically active peptide or its synthetic intermediate. CONSTITUTION:As reagents for removing protecting groups are used (A) an acid selected from methanesulfonic, trichlorosulfonic and trifluosulfonic acids and (B) a thioether derivative of the formula (R ia lower alkyl) as thioanisol preferably in an amount of 4-10 equivalents per one protecting group in one molecule of peptide. The peptide protected with groups is treated with the above reagent preferably at 0 deg.C-room temperature for 0.5-24 hr and both groups protecting carboxyl and amino groups are simultaneously removed.