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Synfacts 2007(10): 1008-1008  
DOI: 10.1055/s-2007-968945
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of (+)-Camptothecin

Contributor(s): Philip Kocienski, Indu Dager
H.-B. Zhou, G.-S. Liu, Z.-J. Yao*
Shanghai Institute of Organic Chemistry and University of Science and Technology of China, Hefei, P. R. of China
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Publication History

Publication Date:
07 November 2007 (online)

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Significance

Isolated from the Chinese plant Camptotheca acuminata, camptothecin exhibits antitumor activities by stabilizing the complex between DNA and topoisomerase I during DNA relaxation. The short and efficient synthesis of (+)-camptothecin (8 steps, 47% overall yield) reported here is a modification of an earlier procedure by Fortunak et al. (Tetrahedron Lett. 1996, 37, 5679).