2. Academic Validation
  3. Selective phenolic acylation of 10-hydroxycamptothecin using poly (ethylene glycol) carboxylic acid

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

  • Bioorg Med Chem Lett. 2003 Feb 10;13(3):577-80. doi: 10.1016/s0960-894x(02)00926-5.
Richard B Greenwald 1,  Yun H Choe,  Dechun Wu
Affiliations

Affiliation

  • 1 Enzon, Inc., 20 Kingsbridge Road, Piscataway, NJ 08854, USA. richard.greewald@enzon.com
PMID: 12565975 DOI: 10.1016/s0960-894x(02)00926-5
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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