李英, 杨正修, 陈一心, 章辛. 15-14C标记青蒿素的合成J. 药学学报, 1994, 29(9): 713-716.
引用本文: 李英, 杨正修, 陈一心, 章辛. 15-14C标记青蒿素的合成J. 药学学报, 1994, 29(9): 713-716.
YLi, zx Yang, YX Chen , x zhang, . SYNTHESIS OF 15-14CLABESED ARTEMISININJ. Acta Pharmaceutica Sinica, 1994, 29(9): 713-716.
Citation: YLi, zx Yang, YX Chen , x zhang, . SYNTHESIS OF 15-14CLABESED ARTEMISININJ. Acta Pharmaceutica Sinica, 1994, 29(9): 713-716.

15-14C标记青蒿素的合成

SYNTHESIS OF 15-14CLABESED ARTEMISININ

  • Abstract: 15-14CArtemisinin(8) was prepared by the biosynthesis of15-14Cdihydroartemisic 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.

     

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