反应详情

To a mixture of 2-(4-((benzyloxy) carbonyl)piperazin-1-yl)-4-bromobenzoic acid (2 g, 9.1 mmol) in THF (20 mL) was added dropwise BH3/THF (1.0 M, 40 mL) at 0° C. The mixture was refluxed for 2 h, then cooled to RT, quenched with H2O, and extracted with ethyl acetate, 3 N HCl, brine, then dried over Na2SO4, filtered and concentrated. Purification by normal phase silica gel (ethyl acetate/hexanes) provided benzyl 4-(5-bromo-2-(hydroxymethyl)phenyl)piperazine-1-carboxylate as a white solid.

1. temperatureThe mixture was refluxed for 2 h
2. customquenched with H2O
3. extractionextracted with ethyl acetate, 3 N HCl, brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated
7. customPurification by normal phase silica gel (ethyl acetate/hexanes)