Synthesis of 2,3-Dihydro-1,4-benzodioxin Derivatives. I. : 2-Substituted-5(and 6)-sulfamoyl-2,3-dihydro-1,4-benzodioxins

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In order to study new sulfonamide diuretics, two series of 6- and 5-sulfamoyl-2,3-dihydro-1,4-benzodioxins were synthesized and tested for diuretic and antihypertensive activities in rats. Starting from 4-chloro(or 3,4-dichloro)-1,2-dihydroxybenzene, these sulfamoyl compounds were prepared by two different routes. In method A, 6-sulfamoyl compounds (8 or 11) were obtained by conversion of the nitro function into sulfonamide via the Sandmeyer reaction. In method B, 5-sulfamoyl compounds (16) were synthesized by direct introduction of sulfonyl chloride into the dihydrobenzodioxin, followed by amination. The sulfamoyl dihydrobenzodioxins showed lower diuretic and antihypertensive activities than trichloromethiazide.
公益社団法人日本薬学会の論文
1988-09-25