Scheme 1.
Reagents and conditions: (a) EDC, DMAP, DCM, DIPEA, 95%; (b) 20% CuI, 5% Pd(PPh3)4, 48 acetylenes (1.1 equiv.), DMF, DIEA, 60 °C, 1 h, 15-90%.
Reagents and conditions: (a) EDC, DMAP, DCM, DIPEA, 95%; (b) 20% CuI, 5% Pd(PPh3)4, 48 acetylenes (1.1 equiv.), DMF, DIEA, 60 °C, 1 h, 15-90%.