| 摘要 |
PURPOSE: Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS) are provided. CONSTITUTION: Provided is a compound represented by formula I, wherein X is O or CH2,and R1 is hydrogen or alkyl and, R2, R3, R4 and R5 are independently hydrogen or lower alkoxy which are useful in treating acute amyotrophic lateral sclerosis (ALS). The compounds of formula I may be synthesized by the following methods: (a) Reaction of an alcohol of the formula RCH2OH with a chlorosulfamate of the formula CISO2NH2 or CISO2NHR1 in the presence of a base such as potassium a-butoxide or sodium hydride at a temperature of about -20 to 25°C and in a solvent such as toluene; (b) Reaction of an alcohol of the formula RCH2OH with sulfurylchloride of the formula SO2Cl2 in the presence of a base such as triethylamine or pyridine at a temperature of about -400 to 25 C in a solvent; (c) Reaction of the chlorosulfate RCH2OSO2Cl with a metal azide such as sodium azide in a solvent such as methylene chloride or acetonitrile yields an azide sulfate of the formula RCH2OSO2N3 as described by M.
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