A new a-ray quantitative measurement method has been proposed, where the measurement system is designed to connect a liquid scintillation counter with a multichannel pulse-height analyzer. This technique provides the remarkable advantages such as a simplicity of sample preparation, a 100% counting efficiency measurement and the elimination of interfering radiations.
2- (4- (2-Thienylcarbonyl) phenyl) propionic acid (suprofen), an anti-inflammatory agent, was labeled with tritium or carbon-14 for the purpose of investigating its metabolic fate in animals. The selectively tritiated suprofen (26.3-32.1 GBq (710-867mCi) lmmol) was obtained by catalytic dehalogenation of the brominated precursor with 185-370 GBq (5-10 Ci) of tritium gas. The labeled position of the suprofen was confirmed by spectral data of the deuterated suprofen similarly synthesized. On the other hand, suprofen-14C (48.8 MBq (1.4 mCi) /mmol) was obtained by five-step synthesis from toluene [methyl-14C] in a 19% yield.
2- (4- (2-Thienylcarbonyl) phenyl) propionic acid (suprofen), an anti-inflammatory agent, was labeled with multiple-deuterium for the purpose of investigating the metabolism in man and animals by the ion cluster technique. Racemic suprofen-d4 was prepared by ten-step synthesis from bromobenzene-d5 in a 32% yield, and its deuterium content was 99 atom%. This racemic suprofen-d4was resolved by use of an optically active a-methylbenzylamine, resulting that optically active suprofen-d4 was obtained in a 11% yield and was 96.5 atom% D. On the other hand, suprofen-d7 (99 atom% D) was obtained by five-step synthesis from toluene-d8 and methyl-d3iodide in a 24% yield.