1H-Indazole → 1H-Benzimidazole-2-carboxaldehyde

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Reaction Steps

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

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