反应详情

Lithium hydroxide (2 mg, 0.077 mmol) in water (0.5 ml) was added into methyl 2-[(4-{2-[(benzylsulfonyl)amino]ethyl}phenoxy)methyl]benzoate (17 mg, 0.038 mmol) dissolved in THF (1 ml). The mixture was then in irradiated in a microwave oven (Smith Synthesizer) at 150° C. for 7 minutes and then evaporated to remove THF. The residue was acidified with 1% hydrochloric acid, pH˜4, and extracted with ethyl acetate (×2). The organic extracts were combined and dried with MgSO4 and then evaporated. Chromatography of the residue on a column (ISOLUTE® SI, 500 mg/3 ml) using DCM, then MeOH/DCM (0.5:99.5) as eluant gave 10 mg the desired product, yield 61%.

1. customin irradiated in a microwave oven (Smith Synthesizer) at 150° C. for 7 minutes
2. customevaporated
3. customto remove THF
4. extractionextracted with ethyl acetate (×2)
5. dry with materialdried with MgSO4
6. customevaporated