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Synthesis of Intermediates 1 and 4a
aReagents and conditions: (a) NaNO2, NaBr, 0.75 M HBr, −15 °C; (b) MgSO4, H2SO4, t-BuOH, rt, 45% for two steps; (c) Boc2O, K2CO3, tetrahydrofuran (THF)/H2O (1/4), rt; (d) EDC.HCl, HOBt, dimethylformamide (DMF), rt, 82% for two steps; and (e) TFA/DCM (1/2), 63%.
