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Synthesis of 2,3,6-trisubstituted-5,6-dihydroimidazo[2, 1-b]thiazole derivatives
(a) Boc-AA-OH (5 equiv), DIC (5 equiv), HOBt (5 equiv); 55% TFA/DCM. (b) BH3·THF (40 equiv), 65 °C, 72 h; piperidine, 65 °C, overnight. (c) 1,1′-thiocarbonyldiimidazole (5 equiv) in CH2Cl2, overnight. (d) α-haloketone (5 equiv) in DMF, 65 °C, 24 h. (e) anhydrous HF, 0 °C, 1.5 h.
