反应详情

To a stored solution of 7-hydroxy-N-(4-(4-phenylbenzoylamino)butyl)-1,2,3,4-tetrahydroisoquinoline (05 g, 1.3 mmol) and triethylamine (0.21 ml; 1.5 mmol) in dichloromethane (20 ml) was added pyridine-3-sulfonyl chloride (0.25 g, 1.4 mmol). The mixture was stirred for 18 h, then partitioned between dichloromethane (4×30 ml) and saturated aqueous NaHCO3 (100 ml). Combined organic extracts were dried (Na2SO4) and evaporated in vacuo to give an oil. Chromatography on silica using 0-5% methanolethyl acetate gradient elution gave the title compound (0.06 g, 12%) as an oil.

1. custompartitioned between dichloromethane (4×30 ml) and saturated aqueous NaHCO3 (100 ml)
2. dry with materialCombined organic extracts were dried (Na2SO4)
3. customevaporated in vacuo
4. customto give an oil
5. washChromatography on silica using 0-5% methanolethyl acetate gradient elution