✍ Scribed by Milton J. Komet
No coin nor oath required. For personal study only.
Several 3‐benzyl‐1,2,3‐benzotriazin‐4(3__H__)‐ones 1 were prepared by alkylation of 1,2,3‐benzotriazin‐4(3__H__)‐one with benzyl halides in dimethylformamide in a microwave oven in moderate yields. Accompanying 1 were minor amounts of products believed to be the O‐alkylated derivatives. Support for 3‐benzylation is shown by an alternate synthesis of la from o‐amino‐N‐benzylbenzamide by nitrous acid cyclization. The title compounds were evaluated in mice and rats in maximal electroshock (MES) and pentylenetetrazole (scMet) seizure models for anticonvulsant activity, and in the rotorod test for neurotoxi‐city. They were generally non‐toxic. The 3‐benzyl analog was the most active (maximal electroshock) compound; it's maximal electroshock ED~50~ value was 93 mg/kg (mouse).
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## Abstract Microwave irradiation of 1(2__H__)‐phthalazinone with benzyl halides and potassium carbonate in dimethyl‐formamide afforded 2‐benzyl‐1(2__H__)phthalazinones in modest yields. These products were tested in mice and rats in maximal electroshock and pentylenetetrazole seizure models for an