| 摘要 |
<p>omega-Sulphamoylalkyl-1,2-benziosoxazole derivs. are of formula (I). In the formula, X is H, halogen (pref. at 5 or 6-position) or CF3. R1 and R2 are H, 1-3C alkyl (pref. methyl, ethyl or isopropyl) or hydroxy (except when R1 and R2 are hydroxyl or = 4-methyl-1-piperazinyl. n is 1-3. A specific (I) is 3-sulphamoylmethyl-1,2-benzisoxazole. (I) and alkali metal salts have anticonvulsant activity. In an example, an ethyl acetate soln. of 1,2-benzisoxazole-3-methanesulphonic acid chloride is ice-cooled and saturated with ammonia gas. The resultant mixture is allowed to stand at room temp. for 1 hr., filtered to remove insolubles and then distilled to remove ethyl acetate. The residue is washed with a small amt. of ethyl acetate and recrystallised from ethyl acetate to give sulphamoyl-methyl-1,2-benzisoxazole, m. pt. 160-163 degrees C.</p> |
