Methyl sulfone (MeSO2) is a standard polar substituent used in chemistry together with methoxy, dimethylamino, acetoxy, and acetyl (Figure ). It is common in agrochemicals, and can be found in structures of >30 drugs. All of them are either aliphatic or aromatic compounds (Figure , see also SI p. S6-S7). Heteroaromatic methyl sulfones, due to the lack of convenient and effective chemical approaches to them, are considerably much less investigated.