Water → HCID 18998817, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-(2-hydroxyprop-1-yl)-4-(6-fluoro-1-methyl-1H -indazol-3-yl)piperidine (200 mg; 0.69 mmol) in 5 ml dry DMF was added 3,4,5-trimethoxyphenylisocyanate (200 mg; 0.96 mmol) in 3 ml dry DMF. The reaction mixture was heated to 100° C. for 2 h, followed by cooling to room temperature and addition of a mixture of 25 ml water and 150 ml ether. The reaction mixture was filtered and separated. The ether phase was washed with water, brine, dried with sodium sulphate and concentrated in vacuo. The crude product was purified by chromatography on silica gel 60 with ethyl acetate:methanol (9:1, v/v) as eluent. Concentration of the appropriate fractions gave 100 mg (29%) of the title compound. M.p. 74°-77° C.

Provenance & Evidence