The process for the simultaneous protection and activation of amino acids

摘要

PURPOSE: A method for preparing amino acid derivatives in which amine group and carboxyl group are protected is provided to enhance carboxyl group reactivity. CONSTITUTION: An amine group of general formula I is protected with trifluoroacetyl groups. A method for preparing amino acid derivatives in which carboxyl groups are protected in a hydroxy imidester form comprises: a step of reacting N-hydroxy succinimide of chemical formula III with trifluoroacetic acid(CF_3COOH) under the presence of trichloromethyl chloroformate of chemical formula II and triethyl amine; and a step of adding amino acid. The reaction is performed at 0~35°C.