| Autor: |
Paleček, Jiří, Dräger, Gerald, Kirschning, Andreas |
| Předmět: |
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| Zdroj: |
Synthesis; 2011, Vol. 2011 Issue 4, p653-661, 9p |
| Abstrakt: |
A multigram batch of the cyclo[Arg-Gly-Asp-D-Phe-Lys] and its N-e-azido derivative was accomplished via solutionphase synthesis using an epimerization-free fragment condensation. The C-terminus of D-Phe was protected as its tert-butyl ester. Fmoc (Arg, Gly, Asp, D-Phe) and Boc (Lys) groups were used to protect all N-α-termini. The Ts and NO2 groups, respectively were chosen to protect the guanidine group. The macrocyclization step (between D-Phe and L-Lys) was carried out under TBTU/HOBt or DPPA condensation conditions. Finally, the e-amino group of the lysine residue was selectively converted into the azido group by a diazotransfer reaction. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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