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.