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Initial attempted one-pot benzimidazole synthesis.
| Entry | Conditions | Yield[a] (5+6) | Ratio (5:6) |
|---|---|---|---|
| 1 | PhCHO (1.0 equiv. added at start of reaction) |
65 % | 50 : 1 |
| 2 | Reflux 1 hour, then PhCHO (1.0 equiv.), then reflux 16 hours |
71 % | 8 : 1 |
| 2 | Reflux 1 hour, then PhCHO (2.0 equiv.), then reflux 16 hours |
85 % | 1 : 1 |
Yield after chromatography (5 + 6 were co-eluted).
