Table 1.
Bench-scale (0.5 mmol) results from selected HTE leads.
entry | ligand | solvent | equiv MeNO2 | L:Pd | P:SM at 5 ha | yield (%)b |
---|---|---|---|---|---|---|
1 | cataCXium POMetB |
THF | 2 | 2:1 | 93:7 | 66c |
2 | cataCXium POMetB |
1,4-dioxane | 2 | 2:1 | 89:11 | 67c |
3 | XPhos | THF | 2 | 2:1 | 67:33 | 42 |
4 | XPhos | 1,4-dioxane | 2 | 2:1 | 59:41 | 81 |
5 | XPhos | 1,4-dioxane | 5 | 2:1 | 90:10 | 85 |
6 | XPhos | 1,4-dioxane | 10 | 2:1 | 90:10 | 92 |
7 | XPhos | 1,4-dioxane | 2 | 1.2:1 | 62:38 | 79 |
Determined by GC.
Yield after column chromatography.
9 h reaction time.