Substrate scope of imine esters^a.

Entry	R	3	Yieldb (%)	drc	eed (%)
1	p-ClC6H4	3a	81	18 : 1	96
2	m-ClC6H4	3b	67	12 : 1	95
3	p-BrC6H4	3c	98	20 : 1	97
4	p-CF3C6H4	3d	96	15 : 1	98
5	Ph	3e	71	10 : 1	94
6	p-MeC6H4	3f	88	15 : 1	92
7e	o-MeC6H4	3g	76	20 : 1	97
8f	m-MeC6H4	3h	72	15 : 1	91
9f	p-MeOC6H4	3i	79	18 : 1	96
10	1-Naphthyl	3j	56	7 : 1	96
11f	2-Naphthyl	3k	98	10 : 1	95
12	2-Thienyl	3l	98	15 : 1	96
13	2-Furyl	3m	58	9 : 1	86
14	Cyclohexyl	3n	72	20 : 1	97

^aUnless otherwise noted, all reactions were carried out with 0.4 mmol 1, 0.2 mmol 2a, 0.01 mmol Cu(i)/L6 and 0.2 mmol of Cs₂CO₃ in 2 mL of Et₂O for 24 h, Cu(i) = Cu(CH₃CN)₄BF₄.

^bIsolated yield.

^cThe dr value was determined by the crude ¹H NMR.

^dee value was determined by HPLC analysis.

^{e t} BuOK was used instead of Cs₂CO₃.

^fThe reaction was run at 20 °C.