Table 1.
Effect of Amine Protecting Group and Catalyst Structure
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entry | PG | equiv. ald. | cat. (R) | % yielda | drb | %eec |
1 | Cbz | 3.0 | 1 (Me) | 66 | 1.2:1 | 82 |
2 | Boc | 3.0 | 1 (Me) | 62 | 1.4:1 | 86 |
3 | Ts | 3.0 | 1 (Me) | 86 | 4:1 | 90 |
4 | Ns | 3.0 | 1 (Me) | 79 | 6:1 | 90 |
5 | Ns | 1.5 | 1 (Me) | 75 | 6:1 | 90 |
6 | Ns | 1.5 | 2 (Bn) | 77 | 9:1 | 92 |
Isolated yield.
Determined by 1H NMR analysis of crude reaction or isolated mixture.
Determined by chiral HPLC analysis of corresponding alcohol; absolute stereochemistry assigned by X-ray crystal structure or by analogy.
Boc = t-butoxycarbonyl, Cbz = carboxybenzyl, Ts = 4- toluenesulfonyl, Ns = 4-nitrophenylsulfonyl.