Synthesis of 10-Hydroxycamptothecin: Evaluation of New Moderators for the Chemoselective Reduction of Camptothecin

Abstract

10-Hydroxycamptothecin is prepared by chemoselective catalytic hydrogenation of the B-ring of camptothecin over PtO₂ with sulfur moderators followed by oxidation using iodobenzenediacetate. New moderators (viz. thioanisole, dimethyl sulfide, diphenyl sulfide, 2-mercapto ethanol), which moderate the hydrogenation of the B- ring of camptothecin, are being explored.

Keywords:

• Camptothecin
• DMSO
• 10-hydroxycamptothecin
• moderator
• thioanisole

ACKNOWLEDGMENTS

The authors thank the management of Dr. Reddy's Laboratories Ltd. for supporting this work, and support from analytical colleagues is highly appreciated.