Urea‐Mediated Regioselective Nitration of (20S)‐Camptothecin

Abstract

A facile and efficient procedure for the regioselective nitration of (20S) camptothecin, using urea mediated reagent system under relatively mild experimental conditions, yielding promising anticancer drug 9‐nitro‐ (20S)‐camptothecin in 40% yield with purity of 94.5% (on HPLC) is being reported.

^#Indian Patent 1559/DEL December 21, 1999.

Keywords:

• Anticancer drugs
• Camptothecin
• Nitration
• 9‐Nitro‐(20S)‐camptothecin

Acknowledgments

We thank Dr. M. C. Wani of Research Triangle Institute Research Triangle Park, North Carolina, 277709, USA, for providing reference standards and Prof. M. Spiteller, University of Dortmund, Dortmund, Germany, for high resolution NMR and HRMS.

Notes

^#Indian Patent 1559/DEL December 21, 1999.