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化学学报
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化学学报 ›› 1981, Vol. 39 ›› Issue (2): 171-178. 上一篇    下一篇

论文

dl-10-羟基喜树碱及dl-10-甲氧基喜树碱的全合成

蔡俊超1, 殷孟光2, 闵爱珠2, 冯大为3, 张薛鑫4   

  1. 1. 中国科学院上海药物研究所;
    2. 上海第五制药厂;
    3. 上海医药工业研究院;
    4. 上海第十二制药厂
  • 投稿日期:1979-02-22 发布日期:2013-06-03

THE TOTAL SYNTHESIS OF DL-10-HYDROXYCAMPTOTHECIN AND DL-10-METHOXYCAMPTOTHECIN

CAI JUN-CHAO1, YIN MENG-GUANG2, MIN AI-ZHU2, FENG DA-WEI3, ZHANG XUE-XIN4   

  1. 1. Shanghai Institute of Materia Medica, Academia Sinica;
    2. Shanghai No.5 Pharmaceutical Plant;
    3. Shanghai Institute of Pharmaceutical Industrial Research;
    4. Shanghai No.12 Pharmaceutical Plant
  • Received:1979-02-22 Published:2013-06-03

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本文详细报道以1',2',3',5'-四氢-5'-氧代-6'-氰基-7'(1-乙氧羰基)丙基-螺(1,3-二噁茂烷-2,1'- 吲嗪)为原料,经6步及5步反应合成dl-10-羟基喜树碱及dl-10-甲氧基喜树碱的方法。合成产品与天然生物碱的薄板层析、紫外光谱、核磁共振谱和质谱均一致。dl-10-羟基喜树碱正在临床试用中。

Detailed procedures of the total synthesis of the less toxic,more effective antitumor camptotheoinoid alkaloids,dl-10-hydrogycamptothecin and dl-10-methogycamptothecin,are described.Based on the previous works on the total synthesis of dl-10-campotheoin (dl-1),the following procedures were devised.