反应详情

Prepared according to representative procedure described in Example 48 above (i.e., acylation) using hydroxy β-lactone 13j (15.0 mg, 0.059 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (14.8 mg, 0.077 mmol), 4-dimethylaminopyridine (8.71 mg, 0.071 mmol), 0.5 mL of xylene were azeotroped in vacuo for 1.0 h. After twelve hours the residue was then dissolved in CH2Cl2 (1.5 mL) and N-formyl glycine (9.12 mg, 0.089 mmol) was added. The resulting mixture was purified twice by chromatography (SiO2, gradient 10-40% EtOAc:hexanes) to afford β-lactone 17f (10.8 mg, 55%).

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