Stereoselectively synthesis and structural confirmation of dehydrodipeptides with dehydrobutyrine

利用脱氢丁酸立体选择性合成和结构确认脱氢二肽

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Abstract

Most of polypeptides containing α,β-dehydroamino acids have important biological activity, so exploration of synthetic method has practical significance. In this paper, dipeptides were prepared from l-threonine by protecting of c-terminal allyl acetate, and condensing reaction with a series of N-Boc amino acid. Then, treatment of dipeptides obtained with DMAP, (Boc)2O and tetramethylguanidine in the acetonitrile occured β-elimination reaction to yield stereoselectively dehydrodipeptides. Structures of dehydrodipeptides were confirmed by (1)H NMR, (13)C NMR and MS. Analysis of (1)H NMR, 2D NMR and crystal structure showed that the dehydrodipeptides were Z-configuration.Graphical abstractDehydrodipeptides were prepared from l-threonine. Their structures were confirmed by (1)H NMR, (13)C NMR and MS.

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