Loratadine → Desloratadine

Participants

Reaction Steps

8-Chloro-6,11-dihydro-11-(1-ethoxycarbonyl-4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (prepare as described in Schumacher, D. P.; et.al., J. Org. Chem. 1989, 54, 2242-4) (2 mmols) in 13% aq. KOH (20 mL) and ethanol (20 mL) is stirred and heated at reflux temperature under argon for 24 hours. The reaction mixture is cooled and extracted with ether. The ether extracts are dried (Na2SO4), filtered and concentrated under reduced pressure to give the crude product. Pure 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine 8 is obtained by chromatography of the crude product.

Provenance & Evidence