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Reagents and conditions: (i) 5-(benzyloxy) −2-bromopyridine, K2CO3, Pd(dppf)Cl2, 1,4-dioxane, H20, 80 °C; (ii) NaOH, EtOH, H20, 80 °C; (iii) N-methoxymethanamine hydrochloride, HATU, DIPEA, DMF, rt.; (iv) MeLi, THF, −78 °C; (v) BBr3, DCM, −78 °C to rt., N2; (vi) formaldehyde, azetidine, THF, H20, 70 °C.
