Scheme 2.
Reagents and conditions: (a) (i) PdCl2(PPh3)2 (5% mol), CuI (3% mol), TEA:THF 1:1, N2, 40 °C, 40 min; (ii) ACN, 100 °C, 90 min, 62%; (b) (i) LiAlH4, THF, N2, 0 °C, 10 min; (ii) DMP, DCM, 0 °C 15 min, rt 90 min, 85%; (c) diethyl (3,5-dimethoxyphenyl)phosphonate, NaH, THF, MW, 120 °C, 30 min, 76%; (d) BBr3, DCM, 0 °C to rt, overnight, 60%; (e) BCl3, TBAI, DCM, N2, 0 °C to rt, 6 h, 35%.
