NA 兼容的亚氨基噻唑烷骨架合成

Iminothiazolines represents a significant class of privileged heterocyclic scaffolds in active molecules. We present a mild, efficient and DNA-compatible method for constructing a iminothiazolidine-focused DNA-encoded library. The method begins with the in situ conversion of DNA-conjugated amines to isothiocyanate intermediates using 1,1-thiocarbonyldiimidazole (TCDI), which then undergoes a cycloaddition reaction with 3-aminooxetane derivatives to produce iminothiazolidine structures. Due to the diversity of N-terminal substitutions of DNA-conjugated amines and 3-aminooxetane derivatives, a valuable library of iminothiazolidine-focused DNA-encoded molecules can be constructed using this method.