中文摘要：

目的合成伊立替康原料药中的两种有关物质。方法 7-乙基-N-氧化喜树碱以喜树碱为起始原料经自由基乙基化反应、N-氧化反应制得;10-（4-哌啶基哌啶）甲酰氧基喜树碱以10-羟基喜树碱为起始原料与4-硝基苯基甲酰氯酯发生酯化反应,再与4-哌啶基哌啶发生胺解反应制得。结果与结论合成了伊立替康原料药质量标准中提及的两种有关物质,其化学结构经1H-NMR、质谱确证,质量分数经HPLC检测在99%以上,可作为伊立替康原料药质量控制的对照品。

英文摘要：

Objective To synthesize the two related substances of irinotecan. Methods 7-ethylcamptothecinN-oxide was synthesized via ethylation and oxidation reactions,and 10-（ 4-piperidinopiperidine） methanoyl camptothecin was synthesized through the reaction of 4-nitrophenyl chloroformate and 10-hydroxycamptothecin. Results and Conclusions The two related substances of irinotecan were synthesized and their structures were verified by1H-NMR and MS. Their purity are all over 99% by the detection of HPLC,and can therefore be used as the reference substances in the quality control of irinotecan.