摘要 |
PROBLEM TO BE SOLVED: To obtain a new pyrrolidone compound useful for studying the kinetics or action mechanism in vivo of nefiracetam by labeling 3H on a specific site on the benzene ring of nefiracetam. SOLUTION: This new pyrrolidone compound is represented by formula I, being obtained, for example, by the following procedure: 1,3-dimethyl-2- nitrobenzene is reacted with iodine and oleum pref. at 80-120 deg.C for 1-15 min to form the corresponding triiodine modification, which, in turn, is reduced with a reducing agent such as tin chloride in a solvent such as chloroform pref. at 10-30 deg.C for 5-10 h into the corresponding triiodoxylidine, which is then reacted with a pyrrolidoneacetic acid halide in a solvent such as dichloromethane pref. at 10-30 deg.C for 10-30 h to form a compound of formula II, which, in turn, is reacted with tritium gas in the presence of a catalyst such as palladium.
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