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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 34, 2004 - Issue 13
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Original Articles

Synthesis of Camptothecin Melantotransferrin (p97) Conjugate Through a Carbamate Bond

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Pages 2415-2424 | Received 03 Mar 2004, Published online: 10 Jan 2011
 

Abstract

Through its 20‐hydroxy group and a carbamate bond, 20(S)‐camptothecin (1) is chemically linked to melanotransferrin (p97). The key step to modify the steric hindered hydroxy group of camptothecin is achieved by using triphosgene/DMAP in DMF and immediately reacting with tert‐butyl 6‐aminohexanoate (8). The novel camptothecin conjugate 4 is a potential agent for chemotherapy of brain tumor.

Acknowledgments

The authors are grateful to Ms. Grace Laliberte, Dr. Pascale Tiger, Dr. Malcolm Kennard, and Dr. Gavin Arthur for help discussions and part of analytic work.

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