Table 1.
Effect of salts on the formation of 14a
Additive | Equivalents | Yield of 14 (%) |
---|---|---|
None | - | 30 |
NaI | 5 | 48 |
10 | 50 | |
KI | 5 | 20 |
10 | 27 |
Reactions were performed by slow addition (syringe pump, 1 h) of a solution of deprotected 13 (27 µmol) in DMF (10 mL) to a solution of BOP (1.5 equiv.), HOBt (1.5 equiv.), the salt, and iPr2NEt (3 equiv.) in 20 mL of DMF at 0 °C.