7-乙基-喜树碱的合成

Synthesis of 7-Ethyl-camptothecin

以喜树碱为原料合成了7 乙基 喜树碱。考察了多种因素对反应的影响,确定了较理想的反应条件:3g喜树碱,4 5mL丙醛,1 8mLw(H2O2)=30%的双氧水,2 5gFeSO4·7H2O,9mLw(H2SO4)=98%的浓硫酸,在2～3℃反应1 5h,粗产品收率88%,以HPLC分析,w(7 乙基 喜树碱)=93 8%。

7-Ethyl-camptothecin was prepared from camptothecin (CPT).Thus,3 g CPT,4.5 mL propionaldehyde,2.5 g FeSO_4·7H_2O,1.8 mL H_2O_2〔w(H_2O_2)=30%〕 and 9 mL H_2SO_4〔w(H_2SO_4)=98%〕 reacted at 2～3 ℃ for 1.5 h to give the raw product in 88.0% yield and of 93.8% purity(by HPLC).