Optimization of site-selective coupling between A and B^a.

Entry	Pd Source	Ligand	Eq. PivOH	% Conv.	3 : 4
1b	Pd(OAc)2	sSPhos	0	0	N/A
2	Pd(OAc)2	sSPhos	0	0	N/A
3	Pd(OAc)2	sSPhos	0.3	48	14 : 1
4	Pd(OAc)2	sSPhos	0.6	56	14 : 1
5	Pd(OAc)2	sSPhos(NBu4)	0.6	78	16 : 1
6	[(Cin)PdCl]2	sSPhos(NBu4)	0.6	100	15 : 1
7	[(Cin)PdCl]2	SPhos	0.6	100	1.2 : 1
8c	[(Cin)PdCl]2	SPhos	0.6	100	1.2 : 1
9d	[(Cin)PdCl]2	sSPhos(NBu4)	0.6	88	16 : 1
10e	[(Cin)PdCl]2	sSPhos(NBu4)	0.6	82	13 : 1

^aRatios and conversions determined by ¹H-NMR analysis with internal standard.

^bTHF as solvent.

^cPotassium 2,4-dimethoxybenzenesulfonate included as additive (20 mol%).

^d6 eq. 2a used.

^e3 eq. 2a used.