| 摘要 |
Title compds. (I)[R=OH, amino, acyl, carboxy, heterocyclic (un) substd. aryl, alkoxy, alkyl, etc.; X=H, halo, alkyl, alkoxy , useful for treatment of glaucoma, were prepd.. Thus, 3-MeOC6H4SH was alkylated with BrCH2CH(OEt)2 to give 3-MeOC6H4SCH2CH(OEt)2. This was cyclized on treatment with BF3 to give 10:1 mixt. of 6- methoxybenzothiophene (II; R1=H) and its 4-MeO isomer. (II) was lithiated, sulfonylated, and treated with aq. NH3 to give sulfamide (II) (R1=SO2NH2), which was demethylated to give 6hydroxy-2- sulfamoylbenzo[b thiophene
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