新規活性チオールエステルを用いるアシル化反応

概要

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Corresponding thiol esters were sought in reactions of N-protected amino acids, 1 H-tetrazole-1-acetic acid or D(-)-O-formylmandelic acid with 2-methyl-1, 3, 4-thiadiazole-5-thiol or 1-methyl-l H-tetrazole-5-thiol in the presence of the condensing agent for the purpose of synthesizing new active thiol esters for use as acylating agents. Five new 2-methyl-1, 3, 4-thiadiazolethiol esters and five new 1-methyl-l H-tetrazole-5-thiol esters were prepared in high yield. These thiol esters were successfully applied as active N-acylating agents to a facile preparation of peptides and cephalosporins.
社団法人日本農芸化学会の論文