Scheme 3. Synthesis of 57.
t-BuOK, 18-crown-6, CH3I, Et2O, 0 °C, 3 h, 43%.
2,4-Dibromo-5-methylpyrimidine, EtOH, RT, 8 h, 70%.
44, Pd(dppf)Cl2 (0.1 equiv), Na2CO3 (4 equiv), dioxane/H2O (4:1), 100 °C, 15 h, 28%.
BCl3, DCM, RT, 30 min, 71%.
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