5-乙基-5-对氟苯甲酰丙基巴比妥酸在兔体内的代谢产物研究

用高效液相色谱法对5-乙基-5-对氟苯甲酰丙基巴比妥酸在家兔体内的代谢物进行了分离,用二极管阵列检测器测定了原药及代谢物紫外图谱,得出代谢物的紫外吸收性质;同时测试了原药及代谢物的质谱,推测出代谢物的可能结构,并用化学方法合成了代谢物对照品,通过核磁和质谱的测定进一步确证了结构。

STUDY ON METABOLITE OF 5-ETHYL-5-(PARA-FLUOROBENZOYLPROPYL)BARBITURIC AND IN RABBITS

The metabolite of 5-ethyl-5-( p-fluorobenzoylpropy)harbituric acid(coded asF-B-1) in rabbit has been separated with HPLC. UV-spectra of F-B-1 and its metabolite obtained withDAD, in combination with EI-MS and CI-MS of F-B-1, its metabolite and their derivatives wereexamined. Possible structure of the metabolite was obtained.Possible metabolic way of F-B-1 is thereduction of carbonyl on the benzene ring with formation of hydroxyl group. This was furtherconfirmed by identity of HPLC and MS behavior of the metabolite and NaBH4 reductive preduct. Inthe structure of the latter, the carbonyl on the benzene ring was reduced, as proved by NMR(lH-NMR and ¹³C-NMR)spectra.