摘要 |
PURPOSE:To prepare a 5-endo-hydroxyl-dicarboxylic acid imide, by reacting the corresponding end-cis-bicyclo[2,2,1]hept-5-ene-2,3-dicarboxylic acid anhydride successively with a concentrated mineral acid, a halogenation agent, and an amine. CONSTITUTION:The compound of formula IV can be prepared by (1) reacting end-cis-bicyclo[2,2,1]hept-5-ene-2,3-dicarboxylic acid anhydride with a concentrated mineral acid (e.g. excess conc. sulfuric acid) in suspended state, (2) reacting the obtained endo-endo compound of formula I with a halogenation agent (e.g. acetyl chloride) under refluxing temperature, and finally (3) reacting with the amine of formula II [Z is CN or N(R4)(R5); R4 and R5 are H, alkyl, or together with N form the group of formula III or IV; n is 2, 3 or 4] in a solvent at refluxing temperature. USE:Intermediate of antiarrhythmic agent and musculotropic antispasmodic agent.
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