Table 1.
Screening of representative catalyst types.[a]
 | |||||
|---|---|---|---|---|---|
| Entry | R | Ligand | Conv. [%][b] | d.r.[b] | Yield [%][c] |
| 1 | H (1a) | 6 | 47 | 92:8 | 36 |
| 2 | H (1a) | 7 | 58 | 94:6 | 41 |
| 3 | H (1a) | rac-binap | >98 | 95:5 | 80 |
| 4 | Me (2a) | 6 | >98 | 91:9 | 76 |
| 5 | Me (2a) | 7 | >98 | 93:7 | 83 |
| 6 | Me (2a) | rac-binap | >98 | 94:6 | 85 |
[a]
Performed under N2 atm.
[b]
Determined by analysis of 400 MHz 1H NMR spectra of unpurified mixtures (±2%).
[c]
Yields of isolated and purified products (±5%; major isomer for entries 1–3 and both isomers for entries 4–6). See the Supporting Information (SI) for details.
