芳(月弟)化合物的制备续报

对氨甲酰苯(月弟)酸及对胍磺酰苯(月弟)酸以二氯化锡还原,分别成为二氯化对氨甲酰苯(月弟)及二氯化对胍磺酰苯(月弟),再与巯基乙酸在碳酸氢钠存在下缩合,生成双羧甲巯基(对氨甲酰苯)(月弟)及双羧甲巯基(对胍磺酰苯)(月弟)。二氯化对氨甲酰苯(月弟)与二巯基丙酸钠作用则成1-对氨甲酰苯基-3-羧基-2,5-二硫间锑五环。这些硫醇(月弟)盐在小白鼠体内对于日本血吸虫病的疗效与酒石酸锑钾相仿。

THE PREPARATION OF ARYLSTIBINOUS COMPOUNDS(CONT'D)

A previous work reported the preparation of several stibinous compounds from p-carboxy-methylmercaptobenzenestibonic acid. Some analogous compounds have been prepared in the present work from p-carbamylbenzenestibonic acid and p-guanylsulphamylbenzenestibonic acid. Both of the stibonic acids were reduced by stannous chloride in hydrochloric acid solution to the corresponding arylstibinous chlorides. Condensation of the latter compounds with thioglycolic acid in the presence of sodium bicarbenate gave bis-carboxymethylmercapto-(p-carbamylphenyl)-stibine and biscarboxymethylmercapto-(p-guanylsulphamylphenyl)-stibine respectively. 1-p-carbamylphenyl-3-carboxyl-2, 5-dithia-1-stibia-cyclo-pentane was formed on interaction of p-carbamylbenzenestibinous chloride with sodium dimercaptopropionate. Pharmacological tests revealed that the arylstibinous mercaptides so formed were valuable schistosomicides.