ELIMINATION OF PROTECTING GROUP OF N-PROTECTED AZIRIDINE DERIVATIVE

摘要

PURPOSE:To obtain an aziridine derivative free from N-protecting group from an N-protected aziridine derivative, without causing the side reactions such as ring- opening reaction of aziridine, by treating the protected derivative with an amine base. CONSTITUTION:An aziridine derivative of formula II free from N-protecting group is prepared by reacting the N-protected aziridine derivative of formula I (R<1> is protecting group, e.g. aralkyloxycarbonyl, alkanoyl, aroyl, etc.; R<2> is H or lower alkyl; R<3> is a group inert to the reaction) with an amine compound (e.g. alkylamine, aralkylamine, etc.) in a solvent such as methanol, THF, chloroform, etc. The obtained compound is especially useful in peptide syntheses.