反应详情

A mixture of 0.3 g of 4-anilinopiperidine, 0. 8 g of the compound obtained in step C of EXAMPLE 4 and 0.69 g of potassium carbonate in 5 ml of acetonitrile is heated at 50-60° C. for 5 hours. The reaction mixture is poured into water and extracted with AcOEt, the organic phase is washed twice with water and with saturated NaCl solution and dried over Mgso4 and the solvent is evaporated off under vacuum. The residue is chromatographed on silica H using DCM and then a DCM/MeOH mixture (96/4; v/v) as the eluent. The product obtained is taken up with a saturated solution of gaseous HC1 in ether and the precipitate formed is wrung to give 0.12 g of the expected product. M.p.=158° C.

1. extractionextracted with AcOEt
2. washthe organic phase is washed twice with water and with saturated NaCl solution
3. customdried over Mgso4
4. customthe solvent is evaporated off under vacuum
5. customThe residue is chromatographed on silica H
6. customThe product obtained
7. customthe precipitate formed