Abstract An improved synthetic approach to tenatoprazole 1 is described. It started from 2, 3, 5??trimethyl??4??nitropyridine??N??oxide 2 with acetic anhydride via rearrangement and hydrolysis to give 3, Chlorination with SOCl2 yielded 2??chloromethyl??3, 5??dimethyl??4?? nitropyridine hydrochloride 4, then 4 condensed with 2??mercapto??5??methoxy imidazole [4, 5?? b] pyridine 5 to give 5??methoxy??2??[(4??nitro??3, 5??dimethyl??2??pyridinyl) methylthio] ...