Table 2.

Optimization of the asymmetric synthesis of 3 a.

Entry[a]	Ligand	Solvent	Yield [%][b]	e.r.[c]
1	L8	THF	15	64:36
2	L11	THF	30	51:49
3	L12	THF	31	50:50
4	L15	THF	40	73:27
5	L18	THF	79	56:44
6	L19	THF	20	76:24
7	L21	THF	15	66:34
8	L24	THF	98	77:23
9[d]	L24	THF	99	80:20
10[d,e]	L24	THF	98	80:20

[a] Reaction conditions: 2 a (0.236 mmol), Pd₂dba₃ (5 mol %), ligand (10 mol % for bidentate, 20 mol % for monodentate), 1 a (0.590 mmol), LiCl (0.283 mmol), H₂O (26 μL), KOtBu (0.472 mmol), solvent (1.18 mL), room temperature, overnight. [b] Determined by ¹H NMR analysis using 2,5‐dimethylfuran as an internal standard. [c] Determined by SFC analysis on a chiral stationary phase. [d] 1 a: 0.826 mmol. [e] PdCl₂ (10 mol %) and L24 (40 mol %) were used instead of Pd₂dba₃.