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Synthesis of DX-03-12. (a) Trityl Chloride, DIPEA, dry DMF, yield = 78%; (b) (2-methoxyphenyl)boronic acid, K3PO4, 14% Pd(PPh3)4, DMF, inert atmosphere, yield = 63%; (c) BBr3, inert atmosphere, dry dichloromethane, yield = 65%; (d) solvent-free melt, yield = 55%; (e) KOH, dry DMF, yield = 71%; (f) hydrazine hydrate, CH3OH; (g) trifluoromethanesulfonylchloride, DIPEA, dry dichloromethane, yield = 67%; (h) AcOH, CH3OH, yield = 86%.
