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. 2023 Jul 7;9(8):1470–1487. doi: 10.1021/acsinfecdis.3c00040

Scheme 2. Synthesis of Imidazo[1,2-a] Heterocycles 8, 11a,b, 12, and 14.

Scheme 2

Reagents and reaction conditions: (i) pyridine-2-carboxaldehyde, tert-butyl isocyanide, Yb(OTf)3, 120 °C, microwave, 40 min; (ii) HBr, H2O, 110 °C, 4 h; (iii) 2-bromo-5-fluoropyridine, NaOtBu, XPhos Pd G2, t-BuOH, 75 °C, 2 h; (iv) HBr, Br2, room temperature, overnight; (v) 2-aminoaryl, Na2CO3, DMF, 85 °C, 18 h; (vi) NCS, ACN, room temperature, 1 h; (vii) POCl3, 1,2-DCA, DMF, 70 °C, 2 h; (viii) NaCNBH3, MeOH, AcOH, room temperature, 1 h.