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Palladium-catalyzed reactions in the synthesis of 3- and 4-substituted indoles. 4

Journal Article · · Journal of Organic Chemistry; (USA)
DOI:https://doi.org/10.1021/jo00278a029· OSTI ID:7196823

4-Bromo-1-tosylindole (1) was converted to tricyclic indole enone 11, a potential intermediate in the synthesis of tetracyclic ergot alkaloids, by a series of palladium-catalyzed processes. Attempts to construct the ergot D ring by the hetero-Diels-Alder reaction of enone 11 and 1-azabutadiene 12 produced not the expected (4 + 2) adduct 13 but the benz(cd)indoline derivative 14 resulting from attack of the aza diene at the indole 2-position. The thermodynamic stability of the naphthol nucleus makes enone 11 generally susceptible to attack at the indole 2-position, as evidenced by the attack of hydride and methyl cuprate nucleophiles at this portion forming indolines 16 and 17, respectively.

OSTI ID:
7196823
Journal Information:
Journal of Organic Chemistry; (USA), Journal Name: Journal of Organic Chemistry; (USA) Vol. 54:17; ISSN JOCEA; ISSN 0022-3263
Country of Publication:
United States
Language:
English