Scheme 1.
Reagents and Conditions: a) HBTU (1.25 eq), DIPEA (1.5 eq), THF, 25 °C, 16 hr; b) NaCO3H (2 eq), Pd(dppf)Cl2 (0.1 eq), 9:1 DMF:H2O, 110 °C, 1.5 hr; c) TFA (20 eq), DCM, 25 °C, 2 hr; d) K2CO3 (2.2 eq), BrCN (1.0 eq), THF, 0 °C, 30 minutes.
Reagents and Conditions: a) HBTU (1.25 eq), DIPEA (1.5 eq), THF, 25 °C, 16 hr; b) NaCO3H (2 eq), Pd(dppf)Cl2 (0.1 eq), 9:1 DMF:H2O, 110 °C, 1.5 hr; c) TFA (20 eq), DCM, 25 °C, 2 hr; d) K2CO3 (2.2 eq), BrCN (1.0 eq), THF, 0 °C, 30 minutes.