Kg. Estep, AN EFFICIENT SYNTHESIS OF 4-HYDROXY-1H-INDOLE-2-CARBONITRILE AND ITS CONVERSION TO DPI-201-106, Synthetic communications, 25(4), 1995, pp. 507-514
A three-step synthesis of 4-hydroxy-1H-indole-2-carbonitrile (3) from
commercially available 1,5,6,7-tetrahydro-4H-indol-4-one (4) via cyana
tion and subsequent halogenation/dehydrohalogenation proceeds in 84% o
verall yield. The conversion of 3 into positive inotrope DPI 201-106 (
1) is also described.