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司帕沙星(Sparfloxacin,AF4140,CAS11087—86—8,5—氨基—1—环丙基—7—(顺—3,5—二甲基—1—哌嗪基—6,8—二氟—1,4—二氢—4—羰基喹啉—3—羧酸,简称SPFX)是一种新发展的喹诺酮衍生物,对革兰氏阳性,阴性菌和许多其它细菌都具有广泛、有效的抗菌作用。为了研究SPFX的分布和代谢,合成了[羰基—~(14)C]SPFX,使用未标记的化合物进行一些试验后,发现放射性标记较易引入羰基碳上,且在新陈代谢过程中可能保持稳定。以高产量成功地合成了标记的SPFX,
Sparfloxacin (AF4140, CAS 11087-86-8, 5-Amino-l-cyclopropyl-7- (cis-3,5-dimethyl-l-piperazinyl-6,8-difluoro -1,4-dihydro-4-oxoquinoline-3-carboxylic acid, abbreviated as SPFX) is a newly developed quinolone derivative which is broad and effective against Gram-positive, -negative and many other bacteria In order to study the distribution and metabolism of SPFX, [carbonyl- ~ (14) C] SPFX was synthesized and some tests using unlabelled compounds showed that radiolabels were easier to introduce on carbonyl carbon and may be involved in the metabolic process Stable. The labeled SPFX was successfully synthesized in high yield,