Selective phenolic acylation of 10-hydroxycamptothecin using poly (ethylene glycol) carboxylic acid

Bioorganic & Medicinal Chemistry Letters
2003.0

Abstract

Selective acylation of the phenolic hydroxyl group of 10-hydroxycamptothecin has been accomplished using phenyl dichlorophosphate. Additional modification of the 10-OH as an ether permits a 20-acyl derivative to be synthesized. This result along with data from a 6-hydroxyquinoline model strongly suggests that powerful intermolecular hydrogen bonding exists in the parent molecule.

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