反应详情

6-(4-Chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizine (Example 17 a, 1.5 g, 5.1 mmol), dissolved in THF (10 ml), is treated with triethylamine (0.7 ml, 0.51 g, 5 mmol). A solution of diphosgene (0.5 g, 2.5 mmol), dissolved in THF (5 ml), is added dropwise to this solution at RT, and it is stirred for 8 h. Benzyl alcohol (abs., 0.52 ml, 0.54 g) and triethylamine (0.7 ml, 0.51 g, 5 mmol) are then added, and the mixture is stirred at RT for a further 48 h. The reaction mixture is partitioned between water (30 ml) and diethyl ether (60 ml), and the ether phase is washed with NaOH (5%, 20 ml). An oily residue is obtained from the THF/ether phase dried using Na2SO4 sicc. after the removal of the solvent in vacuo.

1. additionis added dropwise to this solution at RT
2. stirringthe mixture is stirred at RT for a further 48 h
3. customThe reaction mixture is partitioned between water (30 ml) and diethyl ether (60 ml)
4. washthe ether phase is washed with NaOH (5%, 20 ml)
5. customAn oily residue is obtained from the THF/ether phase
6. customdried
7. customafter the removal of the solvent in vacuo