安徽化工
安徽化工
안휘화공
ANHUI CHEMICAL INDUSTRY
2014年
3期
30-32
,共3页
9-烯丙基-10-羟基喜树碱%合成
9-烯丙基-10-羥基喜樹堿%閤成
9-희병기-10-간기희수감%합성
9-allyl-10-hydroxy camptothecin%synthesis
以10-羟基喜树碱为原料,经醚化反应先合成10-烯丙氧基喜树碱,再经克莱森重排反应得到9-烯丙基-10-羟基喜树碱的初产品。通过对醚化反应时间和温度进行研究,得到了较佳的反应条件,初产品总收率为39.8%,并经过LC/MS,1HNMR进行结构确证,产品纯度达到95%以上,为9-烯丙基-10-羟基喜树碱的合成提供了简便高效的合成方法。
以10-羥基喜樹堿為原料,經醚化反應先閤成10-烯丙氧基喜樹堿,再經剋萊森重排反應得到9-烯丙基-10-羥基喜樹堿的初產品。通過對醚化反應時間和溫度進行研究,得到瞭較佳的反應條件,初產品總收率為39.8%,併經過LC/MS,1HNMR進行結構確證,產品純度達到95%以上,為9-烯丙基-10-羥基喜樹堿的閤成提供瞭簡便高效的閤成方法。
이10-간기희수감위원료,경미화반응선합성10-희병양기희수감,재경극래삼중배반응득도9-희병기-10-간기희수감적초산품。통과대미화반응시간화온도진행연구,득도료교가적반응조건,초산품총수솔위39.8%,병경과LC/MS,1HNMR진행결구학증,산품순도체도95%이상,위9-희병기-10-간기희수감적합성제공료간편고효적합성방법。
Preparation of 9-allyl-10-hydroxy camptothecin by 10-hydroxy camptothecin (HCPT) through etherification and Claeson rearrangement reaction was studied in this paper. The conditions of etherification reaction such as temperature, time were examined. The optical conditions were experimentally selected and the total yield of 9-allyl-10-hydroxy camptothecin is 39.8% with 95% purity. An effective method with mild conditions, is provided for the synthesis of arrays of 9-allyl-10-hydroxy camptothecin.