1-(3-Aminopropyl)-4-methylpiperazine → 2-{5-Methyl-2-[3-(4-methylpiperazin-1-yl)-propylamino]-pyrimidin-4-yl}-benzo[b]thiophene-6-carboxylic acid methyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-(2-chloro-5-methylpyrimidin-4-yl)-benzo[b]thiophene-6-carboxylic acid methyl ester (2.08 g, 6.50 mmol) and 1-(3-aminopropyl)-4-methylpiperazine (3.00 g, 19.0 mmol) in 1,4-dioxane (40 mL) is heated at 90° C. for 20 hours. The solvent is evaporated and the resulting residue is subjected to chromatography on silica gel, eluting with 2M NH3/CH3OH in dichloromethane 0-8%, to give the title compound (1.30 g, 72% yield). ES+(m/z) 460 [M+H].

Provenance & Evidence