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. 2021 Apr 14;64(9):6241–6261. doi: 10.1021/acs.jmedchem.1c00263

Scheme 3. Synthesis of Aminothiophene with Different Amide Substituents 11ad.

Scheme 3

Reagents and conditions: (a) di-tert-butyl decarbonate ((Boc)2O), 4-dimethylaminopyridine (DMAP), Et3N, CH2Cl2, rt, 6 h; (b) 1 mol/L NaOH aqueous solution, CH3OH, reflux, 4 h; (c) alicyclic amines, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI), 1-hydroxybenzotriazole (HOBt), Et3N, DMF, rt, 12 h; (d) trifluoroacetic acid (TFA), CH2Cl2, rt, 2.5 h.