反应详情

温度

45 °C

To a solution of 4-hydroxy-4-benzyl-piperidine (380.6 mg, 2 mmol) in dry THF (10 mL) is added 1-(2-chloro-ethyl)-3-(2-methyl-quinolin-4-yl)-urea (263.7 mg, 1 mmol) and solid NaHCO3 (672 mg, 8 mmol). The reaction mixture is stirred at 45° C. for 6 days. The reaction mixture is diluted with CH2Cl2 (100 mL) and washed with sat. Na2CO3 (2×30 mL). The aqueous phase is re-extracted with CH2Cl2 (2×25 mL), the combined organic phases are washed with brine (20 mL), dried (Na2SO4), filtered and evaporated. The residue is purified by preparative HPLC to provide the title compound.

1. washwashed with sat. Na2CO3 (2×30 mL)
2. extractionThe aqueous phase is re-extracted with CH2Cl2 (2×25 mL)
3. washthe combined organic phases are washed with brine (20 mL)
4. dry with materialdried (Na2SO4)
5. filtrationfiltered
6. customevaporated
7. customThe residue is purified by preparative HPLC