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. Author manuscript; available in PMC: 2020 Mar 18.
Published in final edited form as: Angew Chem Int Ed Engl. 2019 Feb 27;58(12):3923–3927. doi: 10.1002/anie.201814272

Table 1.

Optimization of the Reaction Conditions[a]

graphic file with name nihms-1032677-t0002.jpg
Entry Promoter (20%) Yield[b](%) Enantiomeric Ratio (er)[c]
1 - 12 50:50
2 PA1 74 83:17
3 PA2 69 75:25
4 PA3 29 55:45
5 PA4 69 65:35
6 PA5 73 80:20
7 PA6 72 86:14
8 PA7 90 91:9
9 PA8 79 87:13
10[d] PA7 75 92:8
11[d, e] PA7 74 93:7
12 [d, e] PA9 65 91:9
13 [d, e] PA10 71 94:6
[a]

Reaction conditions: 1a (0.05 mmol), 2a (3.0 equiv), Pd(PhCN)2Cl2 (10 mol %), ligand (20 mol%), anhydrous benzene (0.2 M), 70 °C, 2 days.

[b]

Isolated yield.

[c]

Enantiomeric ratio determined by chiral SFC.

[d]

At 0.1 M concentration.

[e]

At 55 °C, 4 days.