反应详情

Prepared according to representative procedure described in Example 48 above (i.e., acylation) using hydroxy β-lactone 13k (15.6 mg, 0.058 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (14.4 mg, 0.075 mmol), 4-dimethylaminopyridine (8.7 mg, 0.070 mmol), 0.5 mL of xylene were azeotroped in vacuo for 1.0 h. The residue was then dissolved in CH2Cl2 (1.5 mL) and N-formyl glycine (9.0 mg, 0.087 mmol) was added. After twelve hours resulting mixture was purified by chromatography (SiO2, gradient 10-40% EtOAc:hexanes) to afford β-lactone 17g (11.7 mg, 57%).

1. customPrepared
2. customwere azeotroped in vacuo for 1.0 h
3. dissolutionThe residue was then dissolved in CH2Cl2 (1.5 mL)
4. customAfter twelve hours resulting mixture
5. customwas purified by chromatography (SiO2, gradient 10-40% EtOAc:hexanes)