Preparation | N-BOC-6-hydroxy -3, 4-dihydroisoquinoline can be 1,2,3, 4-tetrahydroisoquinoline-6-ol and ditert-butyl dicarbonate are prepared by one-step reaction. 1,2,3, 4-tetrahydroisoquinolin-6-ol (2.0g,13.4mmol) and 4-dimethylaminopyridine (24mg) were added to tetrahydrofuran (60mL), ditert-butyl dicarbonate (3.07mL,13.4mmol) were added dropwise in an ice bath, and then stirred at room temperature for half an hour. After the reaction, spin the solvent under reduced pressure, add dichloromethane for dilution, then wash with saturated sodium bicarbonate solution, the organic layer is dried by anhydrous sodium sulfate, then concentrated under reduced pressure, and separated and purified by column chromatography (petroleum ether: ethyl acetate = 5:1) to obtain white oily N-BOC-6-hydroxy -3, 4-dihydroisoquinoline (2.34g,70%). |