Microwave‐assisted Solid‐phase Synthesis of N‐substituted‐2‐aminobenzo[d][1,3] Thiazine Derivatives from a BOMBA Resin

摘要: An efficient solid-phase methodology has been developed for the synthesis of N-acyl and N-sulfonyl substituted 2-aminobenzo[d][1,3]thiazine derivatives. The key step in this is preparation backbone amide linker-bound resin through cyclization reaction between isothiocyanates BOMBA under microwave irradiation. This core skeleton undergoes substitution reactions with various electrophiles, such as acid halides sulfonyl halides, to generate resins, respectively. Finally, N-sulfonyl-substituted derivatives are prepared good yields purities by cleavage respective resins trifluoroacetic (TFA) dichloromethane (DCM).