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A simple and efficient iodine‐promoted synthesis has been developed for the synthesis of isoxazolyl aryl thiazole amines (3) from easily available isoxazolyl aryl ethanones (1) and thiourea (2) in good yields. Furthermore, isoxazolyl aryl thiazole amines (3) are utilized as building blocks for the synthesis of novel isoxazolyl imidazo[2,1‐b]thiazole libraries 6. All the synthesized compounds were characterized by IR, ¹H NMR, ¹³C NMR, and Mass spectral data. The title compounds 6a‐ah were evaluated for their antimicrobial activity. Compounds 6d, 6 g, 6p, 6q, 6r, 6 s, 6u, 6v, 6w, and 6x exhibited significant antimicrobial activity as that of standard drugs.