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. 2023 Jan 25;66(3):1972–1989. doi: 10.1021/acs.jmedchem.2c01767

Scheme 1. Synthetic Route for Compounds 5aab.

Scheme 1

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.