反应详情

4-(2-Aminoethyl)-piperidine-1-carboxylic acid tert-butyl ester (1.22 g, 5.35 mmol) is added to a stirred suspension of 2-(2-chloro-5-methylpyrimidin-4-yl)-benzo[b]thiophene-4-carboxylic acid cyclopropylamide (0.736 g, 2.14 mmol) and diisopropylethylamine (1.12 mL, 6.42 mmol) in anhydrous 1,4-dioxane (8 mL) at room temperature under nitrogen. The resultant mixture is heated in an oil bath at 97° C. for 48 hours. At room temperature the mixture is concentrated and chromatographed on silica gel, eluting with CH3OH in dichloromethane: 0-4%, to give 4-{2-[4-(4-cyclopropylcarbamoyl-benzo[b]thiophen-2-yl)-5-methyl-pyrimidin-2-ylamino]-ethyl}-piperidine-1-carboxylic acid tert-butyl ester as a solid.

1. concentrationAt room temperature the mixture is concentrated
2. customchromatographed on silica gel
3. washeluting with CH3OH in dichloromethane