化学療法剤の研究(第7報) : ハロゲン置換Diphenylether類の合成と抗微生物性について(有機化学)

概要

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Of the amino compounds used as starting materials, 4-amino-4'-fluorodiphenyl ether (II) and 4-amino-4'-dimethoxydiphenyl ether (IV), other than 4-amino-, 4-amino-4'-chloro-, and 4-amino-4'-bromo-diphenyl ethers, and 4-amino- and 4-amino-4'-chloro-diphenyl sulfides, were obtained by the respective reduction of 4-nitro-4'-fluorodiphenyl ether (I) and 4-nitro-4'-methoxydiphenyl ether (II) with stannous chloride and hydrochaotic acid after formation of I and II, respectively by the reaction of the potassium salt of p-fluorophenol and p-methoxyphenol with p-chloronitrobenzene by the Ullmann method. For the syntheses of A and B type compounds (by A- and B-type reactions), the starting amino compound was reacted with the corresponding halogenoacetyl chloride in xylene or acetic acid to obtain the halogenated diphenyl ethers (V to XXXII). The yield was higher when acetic acid was used as a solvent. Antimicrobial activity of the compounds V to XXXII was examined in vitro, and XV and XXVIII were found to have a strong antifungal activity.
公益社団法人日本薬学会の論文
1972-02-25