Synthesis of Novel Coumarin-7,8-cyclophosphoramide Analogs

Abstract

Coumarin-7,8-cyclophosphoramide derivatives were conveniently prepared by a facile method. 7-Hydroxycoumarin was aminomethylated regioselectively at the 8-C position using the Mannich reaction. The newly formed 8-(N-alkylaminomethyl) coumarins were then coupled with bis-β-chloroethyl dichlorophosphamide to form coumarin-7,8-cyclophosphoramide analogs. An efficient, highly regioselective method to synthesize coumarin-7,8-cyclophosphoramide derivatives is provided, and the approach has the merits of mild reaction conditions.

Keywords:

• Coumarin-7,8-cyclophosphoramide
• cyclophosphoramide
• 7-hydroxycoumarin
• Mannich reaction

ACKNOWLEDGMENTS

We are grateful to the National Science Foundation of China (No. 20472076) and the Henan Science Foundation for Excellent Youth (No. 0512001400) for financial support.