Scheme 4.
Large-scale synthesis of 3-PBC (1) and βCCt (2) using the new route
Reagents and conditions: (a) 5 mol% Pd(OAc)2, 7.5 mol% X-Phos, 1.5 eq. Cs2CO3, toluene, 100°C, 15 h; (b) Pd(OAc)2, (t-Bu)3P.HBF4, K2CO3, DMA, 120°C, 16 h
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