Water → HCID 23504858, compound

Participants

Reaction Steps

To a solution of 1-(6-aminoindan-1-ylmethyl)-4-hydroxy-4-(3-trifluoromethyl-4-chlorophenyl)piperidine, 2j, (6.7 g) and triethylamine (4 mL) in dichloromethane (100 mL) was added dropwise at 0-5° C. a solution of chloroacetylchloride (2.6 mL) in dichloromethane (50 mL). The mixture was stirred overnight at room temperature. Water was added and pH was adjusted to >9. The organic phase was separated and worked up as previously. The crude product was purified by column chromatography on silica gel (eluted with 4% triethylamine in ethyl acetate). Yield of pure 18a 6.2 g as an oil.

Provenance & Evidence