PRODUCTION OF NEW AROMATIC AMINE OR AROMATIC HETEROCYCLIC AMINE UTILIZING CURTIUS REARRANGEMENT REACTION IN SOLID PHASE SYNTHESIS

摘要

PROBLEM TO BE SOLVED: To effectively and rapidly synthesize the subject amine useful as an intermediate for medicaments by utilizing Curtius rearrangement reaction of an aromatic (heterocyclic) carboxylic acid is solid phase.;SOLUTION: This aromatic amine or aromatic heterocyclic amine is obtained by the following process: on (A) solid particles (pref. of p-benzyloxybenzyl alcohol resin), (B) an aromatic carboxylic acid (pref. substituted benzoic acid) or aromatic heterocyclic carboxylic acid (pref. substituted pyridinecarboxylic acid) is reacted with (C) an azide compound (pref. disphenylphosphoryl azide) to effect immobilization of (D) an aromatic substituted carbamate or aromatic heterocyclic substituted carbamate on the component A followed by, as necessary in the presence of a base, reaction of the component D with one or more kinds of reactant selected from alkylating agent, alkenylating agent and aralkylating agent and then isolating and collecting the objective amine from the component A.;COPYRIGHT: (C)2000,JPO