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Further optimization by screening MBH carbonates
| Entry | R/2 | 3 | Yield (%) | dr | ee (%) |
|---|---|---|---|---|---|
| 1 | Me (2a) | 3a | 94 | 3.2:1 | 86/80 |
| 2 | Et (2b) | 3b | 95 | 3.2:1 | 93/91 |
| 3 | Bn (2c) | 3c | 93 | 3:1 | 93/91 |
| 4 | nBu (2d) | 3d | 94 | 2.8:1 | 94/92 |
| 5 | tBu (2e) | 3e | 96 | 2.8:1 | 95/93 |
Reaction conditions: 1a (0.1 mmol), 2 (0.15 mmol), and C4 (10 mol %) in CH2Cl2 (1 mL) at RT for 12 h; Yields refer to isolated yields; The ee values were determined by HPLC analysis on a chiral stationary phase; The dr ratios were determined by 1H NMR.
