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Reagents and conditions: (a) methyl 2-formylbenzoate, DIPEA, sodium triacetoxyborohydride, DCM, 25 °C, 14 h (for 20a); (b) HATU, or COMU, DIPEA, DMF, 25 °C, 2 h; (c) Zn, NH4Cl, EtOH/H2O, 50 °C, 1 h; (d) amine, DIPEA, phenyl chloroformate, DCE 0 °C, 30 min then azetidine, 40 °C, 16 h.
