Table 2. Optimization of reaction conditions.

Entry	BPA	Catalyst a	n	Solvent	Temp. (°C)	e.r. of 2a b	Yield of 2a c (%)
1	3a	Pd(PCy3)2	1.5	Xylenes	140	52 : 48	80
2	3b	Pd(PCy3)2	1.5	Xylenes	140	50 : 50	65
3	3c	Pd(PCy3)2	1.5	Xylenes	140	54 : 46	68
4	3d	Pd(PCy3)2	1.5	Xylenes	140	52 : 48	71
5	3e	Pd(PCy3)2	1.5	Xylenes	140	57 : 43	39
6	3f	Pd(PCy3)2	1.5	Xylenes	140	56 : 44	45
7	3g	Pd(PCy3)2	1.5	Xylenes	140	80 : 20	50
8	3h	Pd(PCy3)2	1.5	Xylenes	140	57 : 43	50
9	3g-[H8]	Pd(PCy3)2	1.5	Xylenes	140	50 : 50	63
10 d	3g	Pd(PCy3)2	1.5	Xylenes	120	87 : 13	24
11	3g	Pd(PCy3)2	3	Xylenes	120	84 : 16	56
12	3i	Pd(PCy3)2	3	Xylenes	120	84 : 16	50
13	3j	Pd(PCy3)2	3	Xylenes	120	55 : 45	15
14	3g	Pd(PCy3)2	3	DME e	120	96 : 4	86
15	—	Pd(PCy3)2	3	DME e	120	—	29
16	3g	Pd2(dba)3	3	DME e	120	—	<2 f
17	3g	Pd2(dba)3/PCy3	3	DME e	120	95 : 5	61
18	3g	Pd2(dba)3/PPh3	3	DME e	120	91 : 9	<20 f
19	3g	Pd2(dba)3/PCyp3	3	DME e	120	97 : 3	24
20	3g	Pd2(dba)3/P(t-Bu)2Me	3	DME e	120	97 : 3	<20 f

^a5 mol% Pd(PCy₃)₂ (entries 1–15) or 2.5 mol% Pd₂dba₃/10 mol% PR₃ (entries 16–20).

^bEnantiomeric ratio measured via HPLC using a chiral stationary phase.

^cYield of isolated product.

^dReaction time: 40 h.

^eWith 4 Å powdered molecular sieves.

^fEstimated based on GCMS ratio. DME = 1,2-dimethoxyethane.