PREPARATION OF PEPTIDE* AND ARGININE DERIVATIVE

摘要

PURPOSE:To prepare a peptide having guanidino group in high yield, by protecting the guanidino group of the starting compound with easily eliminable 4-methoxy-2,6- dimethylbenzenesulfonlyl group. CONSTITUTION:A compound of e.g. formula II (R is H or protecting group of alpha-amine acid) is prepared by reacting a starting compound having a guanidino group of formula I (e.g. arginine) with 4-methoxy-2,6-dimethylbenzenesulfonyl group (usually as a halogenide). The reaction is pref. carried out in a solvent such as water, in the presence of a base, at -10-+25 deg.C. The compound thus obtained is subjected to peptide condensation reaction, and treated with an acid such as trifluoroacetic acid to eliminate the protecting group. The arginine derivative of formula II is a novel compound.