Diethyl Carbonate → (+/-)-3-(1-Methyl-4-piperidyl)-5-(1,3-oxazolidin-4-ylmethyl)-1H-indole

Participants

Reaction Conditions

Reaction Steps

A mixture of the product from step (f) (1.6 g), diethyl carbonate (0.71 g) and potassium carbonate (0.08 g) was heated at 130° C. for 5 hours. The mixture was cooled, taken up in methanol and the insoluble potassium carbonate filtered off. The filtrate was evaporated in vacuo and the residue eluted through a silica column using DCM/EtOH/NH4OH (30:8:1) as eluant to give a colourless foam which was crystallised from isopropanol/ether to give the desired product as a colourless crystalline solid (1.1 g), mp 191°-192° C. 1H NMR and microanalysis as for product of Synthetic Example 4.

Provenance & Evidence