Substrate scope and limitations of three-component auto-tandem reactions^a.

Entry	R	PG	t (h)	Yieldb (%)
1	Ph	Ts	24	4a, 86
2	2-MeC6H4	Ts	24	4b, 93
3	3-MeC6H4	Ts	36	4c, 70
4	4-MeC6H4	Ts	24	4d, 80
5	4-PhC6H4	Ts	24	4e, 79
6	4-FC6H4	Ts	24	4f, 68
7	4-ClC6H4	Ts	24	4g, 74
8	2-Naphthyl	Ts	24	4h, 66
9	2-Furyl	Ts	24	4i, 80
10	2-Thienyl	Ts	36	4j, 72
11	PhCH2CH2	Ts	96	4k, 62
12	c-Hexyl	Ts	96	4l, 23
13	Ph	Ns	96	4m, 52
14c	Ph	Bz	24	4n, 70
15c	Ph	SO2NMe2	24	4o, 90
16d	Ph	Ts	24	4a, 82

^aUnless noted otherwise, reactions were performed with 1a (0.2 mmol), 2a (0.2 mmol), imine 3 (0.1 mmol), Pd(PPh₃)₄ (10 mol%), A2 (40 mol%) and 4 Å MS (40 mg) in degassed dry toluene (1.0 mL) at 70 °C under Ar.

^bYield of isolated product.

^cWith 5a (0.2 mmol) instead of 1a and 2a.

^dOn a 1.0 mmol scale.