APPLICATION OF THE MILD-CONDITION PHTHALIMIDINE SYNTHESIS WITH USE OF 1,2,3-1H-BENZOTRIAZOLE AND 2-MERCAPTOETHANOL AS DUAL SYNTHETIC AUXILIARIES. EFFECTIVE SYNTHESIS OF PHTHALIMIDINES POSSESSING A VARIETY OF SUBSTITUENTS AT 2-POSITION

摘要

The mild-condition phthalimidine synthesis based on Mannich type 1:1 condensation reaction between o-phthalaldehyde with a variety of primary amines in the presence of excess 2-mercaptoethanol and 1,2,3-1H-benzotriazole as "dual synthetic auxiliaries" in MeCN for 13 h at room temperature afford 2-substituted phthalimidines (2,3-dihydroisoindol-1-one) in fair to good isolated yields.