Abstract
An efficient synthesis of the sodium salt of the doxorubicin-peptide conjugate 1, useful for the treatment of prostate cancer is described. The EDC-mediated amide formation between the heptapeptide 4 and doxorubicin (2) as the key step has been extensively studied employing peptide-coupling additives, such as 1-hydroxybenzotriazole (HOBt), 1-hydroxy-7-azabenzotriazole (HOAt) and 2-hydroxypyridine N-oxide (HOPO), surprisingly, mixing the additives HOAt and HOPO furnished the best results.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 647-650 |
| Number of pages | 4 |
| Journal | Synlett |
| Issue number | 5 |
| DOIs | |
| State | Published - 2003 |
| Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Organic Chemistry
Keywords
- Amides
- Coupling reaction
- Isomerization
- Peptide conjugate
- Protecting group
Fingerprint
Dive into the research topics of 'An efficient synthesis of a doxorubicin-peptide conjugate'. Together they form a unique fingerprint.Cite this
- APA
- Author
- BIBTEX
- Harvard
- Standard
- RIS
- Vancouver