Nobuyoshi Haayshi, S. Kato, T. Toga
1975
Citations
0
Influential Citations
2
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The syntheses of disodium 6-(2-phenyl-2-sulfoacetamido-1-14C) peniaillanate (IV) and 6-(2-isobutyl-β,γ- 3H2-sulfo-2-phenyl-acetamido-1-14C) penicillanic acid (XII) are described. The optically active D(-)-IV was obtained by the fractional crystallization of diastereoisomeric mixture which was prepared from phenylacetia acid-1-14C (I). The compound double labelled with 3H and 14C, XII, was synthesized by the reaction of trimethylsilyl 6-aminopenicillanate with 2-isobutyl-β,γ-3H2- sulfo-2-phenylacetyl chloride-1-14C (XI) which was prepared from isobutanol-2,3-3H2 and I. The overall radiochemical yields of XII, at the specific activities of 9 mCi (3H)/mmole and 2 mCi (14C)/mmole, were 34% yield based on isobutanol-2,3-3H2 and 17% yield based on I respeatively.