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. 2019 Jul 11;10:3063. doi: 10.1038/s41467-019-10858-x

Table 2.

Optimization of reaction conditions

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Entry R Cat Solvent Temp/°C Time/h Yield %a ee %b
1 Ph CPA3 DCM(D) −60 12 63 73
2 Ph CPA4 DCM −60 12 24 62
3 Ph CPA5 DCM −60 12 75 74
4 Ph CPA6 DCM −60 12 94 74
5 Ph CPA7 DCM −60 12 58 73
6 Ph CPA8 DCM −60 12 11 12
7 Ph CPA6 Toluene −60 12 24 47
8 Ph CPA6 Et2O(E) −60 12 11 41
9 Ph CPA6 THF −60 12 <2
10 Ph CPA6 D:E = 1:1 −60 12 42 88
11 Ph CPA6 D:E = 7:3 −60 12 67 90
12 Ph CPA6 D:E = 7:3 −70 48 93 91
13 Ph CPA6 D:E = 7:3 −78 48 65 92
14c Ph CPA6 D:E = 7:3 −70 48 94 91

All screening reactions were carried out in a 10 mL glass vial with a PTFE-lined cap on a 0.1 mmol scale. 2.0 equiv of 2a, 10% mol catalyst, 1 mL solvent

aYield represents isolated yield

bDetermined by HPLC analysis

c20 mol% catalyst