PURPOSE: To obtain a sulfamate showing antispasmodic activity and useful for the treatment for symptoms such as epilepsy from an easily available source material under safe conditions.
CONSTITUTION: A compd. expressed by RCH2OH (R is formula I; X is CH2, O; R2 to R5 are H, an alkyl, and when X is O, any groups of R2 to R5 may be bonded to form formula II; R6, R7 are H, an alkyl, or with C to form CR6R7 as a 5 to 6C cycloalkyl ring, however, R6=R7=H is not allowed), especially a compd. expressed by formula III is allowed to react with sulfuryl chloride in the presence of a tertiary or heterocyclic amine base, especially pyridine in a solvent selected from toluene, t-butyl methyl ether(TBME), especially in toluene, to obtain a compd. expressed by RCH2OSO2Cl, especially a compd. expressed by formula IV. Then the obtd. compd. is allowed to react with an amine expressed by the formula; R1NH2 (R1 is H, a 1 to 4C alkyl) in a solvent selected from TBME, THF and lower alkanols, especially in THF to obtain the objective compd. expressed by formula V, especially expressed by formula VI.
ROREIN SUKOTSUTO
KAAKU ERU SOOJI