Table 1.

Optimization of the Reaction Parameters^a

entry	cosolvent [%]b	T [°C]	Pd	conc [M]	yield [%]c	ee [%]d
1	THF	0	Pd(COD)Cl2	0.1	50	85
2	2-MeTHF	0	Pd(COD)Cl2	0.1	61	85
3	2-MeTHF	25	Pd(COD)Cl2	0.1	48	79
4	2-MeTHF	−10	Pd(COD)Cl2	0.1	67	86
5	2-MeTHF	−20	Pd(COD)Cl2	0.1	56	87
6	Tol (30)	−10	Pd(COD)Cl2	0.1	79	86
7	Tol (30)	−10	Pd(COD)Cl2	0.2	76	84
8	Tol (30)	−10	Pd(COD)Cl2	0.05	84	86
9	Tol (30)	−10	Pd(OAc)2	0.05	79	89
10	Tol (30)	−10	Pd(NCPh)2Cl2	0.05	64	86
11	Tol (30)	−10	Pd(dba)2	0.05	72	87
12	Tol (30)	−10	[Pd(ally)Cl]2	0.05	72	88
13	Tol (30)	−20	Pd(OAc)2	0.05	84	89
14	Tol (30)	−30	Pd(OAc)2	0.05	87	91
15	Tol (30)	−40	Pd(OAc)2	0.05	80	91
16	Tol (30)	−30	Pd(OAc)2	0.05	63	91e
17	Tol (30)	−30	Pd(OAc)2	0.05	92	92f

^[a]Reactions performed using 1.0 equiv. of 1a and 2 equiv. of 2a on a 0.1 mmol scale.

^[b]Cosolvent indicates 30% toluene by volume in 2-MeTHF

^[c]Yields determined by ¹H NMR analysis of crude mixtures with CH₂Br₂ as internal standard.

^[d]The ee was determined by chiral SFC

^[e]0.5 equiv. PMDTA was used.

^[f]1.5 equiv. PMDTA was used.