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We have developed an expedient approach,“HOPE”(hybrid orthogonal protocol with ease) strategy for the synthesis of peptidyl N-alkylamides.This new strategy was characterized by following points:incorporating Boc and Fmoc protocols together on Merrifield resin,removal of SPG(side-chain protecting groups) without the damage of linker structure on the resin,and the ammonolysis of linker as the last step could achieve the introducing N-alkylamide structure into C-terminal and releasing product from resin-support simultaneously.In present work,eight peptidylamides with different alkylsubstitution at C-terminal were conveniently synthesized by HOPE strategy.
“We have developed an expedient approach,” “HOPE” (hybrid orthogonal protocol with ease) strategy for the synthesis of peptidyl N-alkylamides. This new strategy was characterized by the following points: incorporating Boc and Fmoc protocols together on Merrifield resin, removal of SPG (side-chain protecting groups) without the damage of linker structure on the resin, and the ammonolysis of linker as the last step could achieve the introduction N- alkylamide structure into C-terminal and product from resin-support. Present work, eight peptidylamides with different alkylsubstitution at C-terminal were adapted synthesized by HOPE strategy.