Hydrochloric Acid → HCID 131721073, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2 g of the compound obtained in step B of EXAMPLE 9, 0.67 g of 4-phenylpiperidine and 1.43 g of potassium carbonate in 6 ml of acetonitrile and 6 ml of DMF is heated at 80° C. for 4 hours. The reaction mixture is concentrated under vacuum, the residue is extracted with AcOEt, the organic phase is washed three times with water and with saturated sodium chloride solution and dried over Na2SO4 and the solvent is evaporated off under vacuum. The residue is chromatographed on silica using a DCM/MeOH mixture (from 100/1; v/v to 100/3; v/v) as the eluent. The product obtained is dissolved in DCM, acidified to pH 1 by the addition of a saturated solution of gaseous HCl in ether and concentrated under vacuum to give 0.39 g of the expected product after crystallization from pentane. M.p.=126°-130° C.

Provenance & Evidence