摘要
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 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.
