YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Biological Changes of p-(Aminoethyl)-phenylsulfonyl Compounds
Tsutomu MomoseMunemitsu Tomoeda
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1952 Volume 72 Issue 12 Pages 1614-1616

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Abstract
Biological changes of p-(α-aminoethyl)-phenylsulfonamide (I), p-(α-aminoethyl)-phenyl methyl sulfone (II), p-(β-aminoethyl)-phenylsulfonamide (III), and p-(β-aminoethyl)-phenyl methyl sulfone (IV) in rabbit were observed by the direct injection of the aqueous solution of the hydrochlorides of these compounds into rabbit stomach by Nela-ton's catheter. The urine was collected about 40 hours after injection, and extracted with ether or ethyl acetate at an optimum pH. Unchanged, free bases of (I) and (II) were obtained in 57% and 26% yield, respectively, and a very small amount of the acetylated compound of (I). (III) and (IV) yielded oxidation products, p-(carboxymethyl)-phenylsulfonamide and p-(carboxymethyl)-phenyl methyl sulfone in 58% and 55% yield, respectively. The free bases of these compounds were not recovered These results led to the conclusion that the oxidation of aminomethyl group was interfered by the introduction of a methyl group into the α-position of the amino radical.
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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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