tert-Butyl piperazine-1-carboxylate → 1-(Phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole hydrochloride

Participants

Reaction Steps

4-(Bromomethyl)-1-(phenylsulfonyl)-1H-indole Intermediate 2 (1.025 g), NaHCO3 (1.5 eq) and N—BOC-piperazine (1.5 eq) were refluxed in ethanol for 40 min. The reaction was monitored by TLC (eluent-system CHCl3-EtOH 20:1). The work up of the crude-extraction and further purification by column chromatography (eluent —CHCl3)—yielded the final product as an oil. This material was treated with HCl 5M in i-PrOH to yield the salt of the final product (300 mg, 24%). The synthetic route followed for preparing Example 1 is depicted in the following scheme:

Provenance & Evidence