【摘要】 <正> 根据一些抗疟药的构效关系,郑贤育等人合成了2-甲氧基-7-氯-10-[3′,5′-双(四氢吡咯次甲基)-4′-羟基苯胺基]苯骈[b]1,5-萘啶四磷酸盐,定名磷酸咯萘啶。磷酸咯萘啶为高效、低毒、与氯喹无交叉抗药性的疟原虫红内期裂殖体杀灭剂。为了进一步研究其在体内的吸收、分布和排泄过程,为临床合理用药提供依据,本文介绍了气液催化交换法制备氚标记磷酸咯萘啶。更多还原

【Abstract】 Pyronaridine is a high efficient and low toxic new antimalarial drug. 3H-pyronaridine was prepared by catalytic isotopic exchange in solution with tritium gas using PdO/BaSO4 as catalyst. That crude product was purified by extraction. 3H-NMR spectra of pyronaridine showed that tritium was labelled at the 6-position. specific activity of 3H-pyronaridine was 5.5 Ci/mmol and radiochemical purity over 95%.更多还原