In this study, a ring-closing metathesis (RCM) synthesis strategy was used to introduce a spirocycle functional group at the 5-position of CPT. The resulting 5-spirocycle CPT compound was obtained with a yield of 73%.
Camptothecin (CPT) is an important natural product targeting to Topoisomerase I (Topo I). Despite the high antitumor activity, this compound cannot enter clinical trial owing to its high toxicity and low bio-availability. In this project, the ring-closing metathesis (RCM) synthesis strategy was employed to introduce spirocycle functional group in the 5-position of CPT. Thus, in the catalysis of Grubbs II catalyst, 5,5-diallylcamptothecin underwent RCM reaction to give 5-spirocycle CPT compound in 73% yield.
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