Indole → Indole-2-carboxaldehyde

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Reaction Steps

In Step 1 of Scheme F, indole compound a is treated with the Vilsmeier reagent formed by mixing oxalyl chloride with dimethyl formamide to form indole aldehyde w, which in turn is reacted with Meldrum's acid in Step 2 to yield indole compound x. Indole x is then treated with Grignard reagent y in Step 3 to afford indole compound z. In Step 4 compound z is reacted with amine d in the presence of pyridine to give indole amide r, which is then reduced in Step 5 to provide aminopropyl indole compound s. Compound s is a compound of formula I in accordance with the invention.

Provenance & Evidence