Hydrochloric Acid → HCID 66810929, compound

Participants

Reaction Steps

A solution of 1-[1-(6-chloro-1H-indole-3-carbonyl)-piperidin-4-yl]-1,3-dihydro-indol-2-one (1 eq) in dry DMF was treated with NaH (1.1 eq) at 0° C. for 60 min. and then a solution of 2,2-dioxo-2λ6-[1,2,3]oxathiazolidine-3-carboxylic acid tert-butyl ester (1.1 eq) and triethylamine (1.1 eq) in dry DMF was added and the mixture stirred at RT for 2 h. After concentration the mixture was treated with 4 M HCl in dioxan (5 eq) at 50° C. for 1 h, evaporated to dryness and partitioned between ethyl acetate and 1 N NaHCO3. The organic layer was washed with brine, separated, evaporated and the crude product chromatographed on silica gel (CH2Cl2-MeOH) to give the title compound.

Provenance & Evidence