反应详情

温度

20 °C

To a solution of 2-methyl-azetidine-1,2-dicarboxylic acid 1-tert-butyl ester 2-ethyl ester, Intermediate 11 (1 eq.) in EtOH was added an aqueous solution of 2N NaOH (2 eq.). The reaction was stirred at 20° C. for 15 h. The solvent was removed under reduced pressure and the crude was partitioned between water and EtOAc. The organic layer was discarded and the aqueous layer was acidified by addition of a solution of citric acid 10% in water until pH=3 and thoroughly extracted by EtOAc. The organic layers were combined, dried over MgSO4, filtered and concentrated under reduced pressure to afford 2-methyl-azetidine-1,2-dicarboxylic acid 1-tert-butyl ester.

1. customThe solvent was removed under reduced pressure
2. customthe crude was partitioned between water and EtOAc
3. additionthe aqueous layer was acidified by addition of a solution of citric acid 10% in water until pH=3
4. extractionthoroughly extracted by EtOAc
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated under reduced pressure