Formamide → Alosetron

Participants

Reaction Steps

A mixture of 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyloxazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one (100 mg) in formamide (20 ml) was heated at 180° for 24 h. The mixture was then cooled, diluted with water (100 ml) and extracted with dichloromethane (3×100 ml). The combined organic extracts were concentrated in vacuo and the residue was purified by FCC eluting with System A (100:8:1) to give the title compound (40 mg) as a solid. The 1H-n.m.r. and t.l.c. data for this material were consistent with those obtained for the product of Example 20.

Provenance & Evidence