1-(3-Aminopropyl)-4-methylpiperazine → [4-(Benzo[b]thiophen-2-yl)-pyrimidin-2-yl]-[3-(4-methylpiperazin-1-yl)-propyl]-amine tri-hydrochloride

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Reaction Steps

1-(3-Aminopropyl)-4-methylpiperazine (3.02 g, 19.2 mmol) is added to a stirred suspension of 4-(benzo[b]thiophen-2-yl)-2-chloro-pyrimidine (2.06 g, 8.34 mmol) in anhydrous 1,4-dioxane (25 mL) at ambient temperature under nitrogen. The resultant mixture is heated in an oil bath at 95° C. for 28 hours. At ambient temperature the mixture is concentrated and subject to chromatographic purification on silica gel, eluting with 2 M NH3/CH3OH in dichloromethane 0-6%, to give the free base of the title compound as a white solid (2.83 g, 92% yield).

Provenance & Evidence