反应详情

A solution of tert-butyl 7-[(2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate (from step (ii) above; 1.0 g, 2.47 mmol) in ethyl acetate (13 mL) was cooled to 0° C. Ethyl acetate (26 mL) saturated with gaseous HCl was added, and the mixture stirred for 4 h at rt. The solvent was removed in vacuo before MeCN (25 mL), water (1.3 mL) and K2CO3 (2.0 g) were added. The resulting mixture was stirred overnight before CHCl3 was added, and the mixture filtered through Celite®. The filtrate was concentrated in vacuo to give 682 mg (91%) of the title compound.

1. customThe solvent was removed in vacuo before MeCN (25 mL), water (1.3 mL) and K2CO3 (2.0 g)
2. additionwere added
3. stirringThe resulting mixture was stirred overnight before CHCl3
4. additionwas added
5. filtrationthe mixture filtered through Celite®
6. concentrationThe filtrate was concentrated in vacuo