New Environmental Benign Approach and Biomimetic Preparation for Natural Scaffold of 2-acyl-thiazole-4-carboxylate
2-acyl-thiazole-4-carboxylates are the key scaffolds in natural tubulysin and ITE families with excellent anti-tumor activity,along with bacillamides as potential algaecides.Various classical designs were carried out for their synthesis instead of rare natural resources,which were restricted by the complicated routes with low yields under relatively harsh conditions.An environmental benign approach was achieved for biomimetic preparation of the crucial skeleton.This article combines the latest source pathway,biomimetic improvement of key oxidative dehydrogenation steps,efficient preparation of this type of intermediate,and preliminary elucidation of the corresponding mechanism,providing novel strategies for its industrial production.