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Synthetic strategy. a) i) Diethyl malonate, NaOMe, n‐PrOH, reflux (105 °C) overnight, 52–99 %. ii) MeOH, pyridine cat., 60 °C, 2 h; or H2O, reflux, 1 h (K2CO3, MeOH, r.t., 2 h when TMS‐alkynyl is used); or AcOH, 15–60 min, 7–25 %. b) i) 1) 3‐Fluoro‐/Bromoaniline, 20 min mechanical mixing, 61–74 %. ii) Malonic acid, POCl3, CHCl3, reflux, 48 h, 60–70 %. iii) 5‐((Trimethylsilyl)ethynyl)furan‐2‐carbaldehyde, H2O, reflux, 1 h then, K2CO3, MeOH, r.t., 2 h, 13 %.
