Three- and Four-Component Syntheses of 3-Arylmethylindoles by Microwave-Assisted One-Pot Heck Isomerization-Fischer Indolization (Alkylation) (HIFI and HIFIA) Sequences

Initiated by Heck isomerization of aryl bromides and allyl alcohols, the intermediate 3-arylpropanal is readily transformed into 3-arylmethylindoles by Fischer indole synthesis in a consecutive three-component fashion in moderate to good yields. This Heck isomerization-Fischer indolization (HIFI) sequence can be readily concatenated into a four-component Heck isomerization-Fischer indolization-alkylation (HIFIA) synthesis affording products in good to excellent yields.