【摘要】 １５－￣１４Ｃ标记青蒿素的合成李英，杨正修，陈一心，章辛（中国科学院上海药物研究所２０００３１）青蒿素是从菊科植物黄花蒿（Ａｒｔｅｍｉｓｉａ，ａｎｎｕａＬ．）中分离到的带有过氧基团的倍半萜内酯。青蒿素及其衍生物对各种疟疾（包括抗氯喹恶性疟和脑型疟）有...更多还原

【Abstract】 C]Artemisinin(8 ) was prepared by the biosynthesis of[15-14C]dihydroartemisic acid(14) which was synthesized from diketone in 6 steps. A supernatant liquidprepared from the tender leaves of ripe Shanghai Qinghao(Artemisia annua L.)was incubated with themixture of compounds l3 and l4(100 mg, total activity 3. 26 MBq, 13:14=1:1) at 30℃or 37℃for 4 hr. After the addition of natural artemisinin(100 mg) ,the mixture was heated at l00℃for5min , and extracted with chloroform(method A)or petroleum ether(bp. 60～90℃, method B).Theextract was evaporated and the residue was recrystallized(method B)or purified py preparative thinlayer chromatography(methed The crude product was recrystallized from methylene chloride Petroleum ether to yield 8 with constant specific radioactivity. The mean rate of incorporation in runs1～8was l.17%。The possible influence factors of the biotransformation were studied. The incuhation temperaturewas considered as a key factor.更多还原