反应详情

To a solution of 4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-1-[1-(2-chloro-pyrimidin-4-yl)-piperidin-4-ylmethyl]-piperazin-2-one (0.40 g, 0.74 mmol) in EtOH is added ethanolamine (0.089 mL, 1.5 mmol). The solution is heated to reflux for 18 h and evaporated to dryness. The residue is chromatographed eluting successively with 1%, 2% and 4% MeOH in CH2Cl2. Fractions containing only product are combined and the solvent evaporated. Trituration with ether afforded the title compound as a yellow solid: MS (ESI): m/z 565 (M++H).

1. temperatureThe solution is heated
2. temperatureto reflux for 18 h
3. customevaporated to dryness
4. customThe residue is chromatographed
5. washeluting successively with 1%, 2% and 4% MeOH in CH2Cl2
6. additionFractions containing only product
7. customthe solvent evaporated