The backbone N-(4-azidobutyl) linker for the preparation of peptide chimera.
2013
A robust synthetic strategy for the introduction of the N-(4-azidobutyl) linker into peptides using standard SPPS techniques is described. Based on the example of Cilengitide it is shown that the N-(4-azidobutyl) group exerts similar conformational restraints as a backbone N-Me group and allows conjugation of a desired molecule either via click chemistry or—after azide reduction—via acylation or reductive alkylation.
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