反应详情

温度

120 °C

To a solution of 4-[7-(2-methanesulfonyloxy-ethoxy)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester (40.6 mg, 0.09 mmol) in DMSO (0.4 mL) was added (S)-(+)-2-pyrrolidinemethanol (90.9 mg, 0.9 mmol). The mixture was stirred at 120° C. overnight and subsequently partitioned between EtOAc and water. The combined organic extracts were washed with brine, dried over Na2SO4 and evaporated. The residue was treated with 50% TFA/CH2Cl2 (8 mL) for 2 h, the solvents (TFA/CH2Cl2) were removed under reduced pressure to provide the desired product. LC-MS (ESI) calcd for C20H29N4O2 (MH+) 357.2, found 357.2.

1. customsubsequently partitioned between EtOAc and water
2. washThe combined organic extracts were washed with brine
3. dry with materialdried over Na2SO4
4. customevaporated
5. additionThe residue was treated with 50% TFA/CH2Cl2 (8 mL) for 2 h
6. customthe solvents (TFA/CH2Cl2) were removed under reduced pressure