DERIVATIVES OF TETRAHYDRO-1,4-BENZODIAZEPIN-5-ONES AND SOLID-PHASE SYNTHESIS METHOD THEREOF

摘要

A manufacturing method of novel tetrahydro-1,4-benzodiazepin-5-one derivative and solid-phase thereof is provided to improve the purity and yield of compound through the single step conversion, thereby simultaneously manufacturing various kinds of compound libraries. The manufacturing method of tetrahydro-1,4-benzodiazepin-5-one derivative represented by the formula(1) comprises the steps of: reacting bromoacetal resin with primary amine to prepare secondary amine; coupling the secondary amine with anthranilic acid in which R3 is substituted; reacting the reaction product with aldehyde or ketone; and reacting the reaction product with formic acid to induce intramolecular cyclization.