Hydrochloric Acid → Lurosetron

Participants

Reaction Steps

A stirred solution of 4-[(6-fluoro-2,3,4,5-tetrahydro-5-methyl-1-oxo-1H-pyrido [4,3-b]indol-2-yl)methyl]-N,N,5-trimethyl-1H-imidazole-1-sulphonamide (92 mg) in absolute ethanol (5 ml) was treated with 2N hydrochloric acid (20 ml) and stirred under nitrogen at 100°-110° for 6 h, and then cooled. 2N Sodium hydroxide (60 ml) was added, and the mixture was extracted with ethyl acetate (2×75 ml). The combined, dried organic extracts were concentrated in vacuo to give a solid (71 mg) which was purified by FCC eluting with System A (100:8:1) to give the title compound (57 mg), m.p. 233°-234°.

Provenance & Evidence