Table 1.
| ||||||
---|---|---|---|---|---|---|
entry | 1 | L | solvent | conv. (%)b |
anti:synb | erc |
1 | 1b | L1 | DMSO | >95 | 3:1 | >99.5:0.5 (98.5:1.5)d |
2 | 1b | L2 | DMF | >95 | 14:1 | 99:1 |
3 | 1b | L2 | DMSO | >95 | 20:1 | >99.5:0.5 |
4 | 1b | L3 | DMF | >95 | 22:1 | >99.5:0.5 |
5 | 1b | L3 | DMSO | >95 (93)e | 29:1 | >99.5:0.5 |
6 | 1a | L3 | DMSO | >95 (91)e | >30:1 | >99.5:0.5 |
7 | 1c | L3 | DMSO | 19 | – | – |
Reactions performed on 0.155 mmol scale;
Determined by 31P NMR analysis of the crude reaction mixture;
Determined by chiral HPLC analysis;
Syn isomer;
Isolated yield.