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| entry | coupling reagent | base | 4a (%) | 2a (%) |
|---|---|---|---|---|
| 1 | HATU | triethylamine | 86 | <1 |
| 2 | HBTU | triethylamine | 84 | 4 |
| 3 | HATU | 2,6-lutidine | 87 | 0 |
| 4 | HBTU | 2,6-lutidine | 83 | 0 |
Yields determined by GC-FID using mesitylene as an internal standard.
