Table 1.

Screening directing groups^a

DGs	Conditions	Conv.b	Yieldb
1a-1e	MeCN, 120 °C	<5%	<5%
1a	L-Proline 20%, MeCN, 120 °C	70%	60%
1b-1e	L-Proline 20%, MeCN, 120 °C	<10%	<10%
1a	Pyrrolidine 20%, Tol, 80 °C	100%	99%(94%c)

^aReaction conditions: 1a (1 eq.), 2a (3 eq.), Pd(OAc)₂ (10 mol%), [amine] cat. (20 mol%), AcOH (1 eq.), solvent (0.5 M), 36 hours.

^bConversion and yield were determined by ¹H NMR using 1,3,5-trimethoxybenzene as internal standard.

^cIsolated yield.