Reagents and conditions: (a)
Pd(dba)2, xantphos, Cs2CO3, dioxane,
110°C, 2 h, 89%; (b) HCl/EtOAC, 15°C, 2 h; (c) tetrahydropyran-4-one,
tetramethylammonium, triacetoxyboranuide, TFA, DCM, 15°C, 2 h;
(d) acetaldehyde, tetramethylammonium, triacetoxyboranuide, TFA, DCM,
15°C, 2 h; (e) TFA, DCM, 45°C, 2 h, 14% (3 steps).