Scheme 1. Synthetic Route for Compounds 5a–ab.

Reagents and conditions: (a) acetyl chloride, AlCl3, dichloromethane, 0 °C to room temperature (rt), 48 h; (b) dibromoethane, NaH, dimethylformamide (DMF), 60 °C, 40 min; (c) 2-bromoethyl 4-methylbenzenesulfonate, Cs2CO3, DMF, rt, 16 h; (d) amine, iso-propyl alcohol (IPA), microwave 100 °C, 30–90 min; (e) amine, DMF, microwave 100 °C, 30 min; and (f) trifluoroacetic acid (TFA), dichloromethane, rt, 1 h.