Protection of histidine in peptide synthesis: A Reassessment of the trityl group

Add time:07/17/2019    Source:sciencedirect.com

The trityl (Trt) group is ideally suited for the side-chain protection of His in peptide syntheses, in combination with 9-fluorenylmethyloxycarbonyl (Fmoc) in Nα- and protecting groups cleavable by mild acidolysis in other positions of the peptide. 2,4,5-trichlorophenyl (Tcp)- and pentafluorophenyl (Pfp)-esters of Fmoc-His(Trt)-OH and Trt-His(Trt)-OH are strongly activated, but stable compounds. Nα-Trt is selectively removable in the presence of NIm-Trt.

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