SYNTHESIS OF 5-(1, 3, 3-TRISUBSTITUTED) INDOLINYL-N,N-DIMETHYLCARBAMATES AS REVERSIBLE CHOLINESTERASE INHIBITORS

In order to study the structure-activity relationship of cholinesterase inhibitor-carbamates, nine 5-indolinyl N,N-dimethylcarbamates have been synthesized as anticholinesterase agents. All compounds tested are strong cholinesterase inhibitors. The pI₅₀ of compound Ⅱa (R=C₄H₉) is 8.26, more potent than CUI XING NING (R=CH₃). For synthesizing these compounds, the technique of phase transfer catalysis was successfully applied in the N-alkylation of oxindoles and the carbamylation of 5-hydroxyindolines.