(1-benzylpiperidin-4-yl)thiourea

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: To a stirred solution of (1-benzyl-piperidin-4-yl)-thiourea (0.5 g, 2.0 mmol) (prepared by a procedure similar to that described in WO 03/062215) in ethanol (15 ml) was added 3-bromo-1,1,1-trifluoroacetone (0.22 ml, 2.1 mmol) and the reaction mixture was heated at reflux for 1 h. After evaporation of the solvent, the crude product was crystallized from acetonitrile to yield D8 (0.61 g, 88%) as a white solid. C16H18F3N3S.HBr free base requires 341. Found 342 (MH+). the reaction mixture was heated at reflux for 1 h After evaporation of the solvent the crude product was crystallized from acetonitrile