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. 2020 Oct 2;142(41):17334–17339. doi: 10.1021/jacs.0c09177

Table 1. Optimization Studies.

graphic file with name ja0c09177_0006.jpg

entry Conditions 4 yield (%)a e.e. (%)
1 Ligand L1, L2 or L3 <5
2 Ligand L4 44 20
3 Ligand L5 33 30
4 Ligand L6 72 40
5 Ligand L7 49 64
6 Ligand L8 45 74
7 Ligand L9 >95 90
8 L9, EtOAc instead of Et2O 80 84
9 L9, MTBE instead of Et2O 89 89
10 L9, Toluene instead of Et2O 91 91
11b L9, 0.40 mmol of 1 >95 94
a

NMR yields.

b

Reaction performed using 1.25 mol % of Pd2(dba)3·CHCl3 and 3.5 mol % of (S,S)-ligand.