反应详情

Ethyl 4-(S)-benzyloxycarbonylamino-4-cyclopropyl-2-butenoate was dissolved in dry nitromethane (15 ml), and the solution was mixed with 1,1,3,3-tetramethylguanidine (133 μl, 1.05 mol) and stirred at room temperature for 17 hours. The reaction solution was concentrated under a reduced pressure, the resulting residue was dissolved in chloroform (50 ml), and the solution was washed with 10% citric acid aqueous solution (50 ml) and saturated sodium chloride aqueous solution (50 ml) in that order, and then dried over anhydrous magnesium sulfate, thereby obtaining 1.207 g (96.1%) of the title compound as a yellow oil. This product (diastereomer mixture) was used in the subsequent reaction without purification.

1. concentrationThe reaction solution was concentrated under a reduced pressure
2. dissolutionthe resulting residue was dissolved in chloroform (50 ml)
3. washthe solution was washed with 10% citric acid aqueous solution (50 ml) and saturated sodium chloride aqueous solution (50 ml) in that order
4. dry with materialdried over anhydrous magnesium sulfate