反应详情

温度

20 °C

Carbonyldiimidazole (10.5 mg, 1.3 eq) in solution in chloroform (0.2 ml) is added to a solution of 2-[(3,5-dimethoxyphenyl)amino]-1-{3-[methyl(2-pyridin-2-ylethyl)amino]propyl}-1H-benzimidazole-5-carboxylic acid (24 mg, 1 eq) in a mixture of dimethylformamide (0.2 ml) and tetrahydrofuran (0.4 ml). The mixture is stirred for 15 hours at approximately 20° C. then thiophene-2-ethylamine (13 mg, 2 eq) in solution in tetrahydrofuran (0.1 ml) is added. After stirring for 15 hours at approximately 20° C., aminomethyl polystyrene resin (2 eq), TBD-methyl polystyrene resin (2 eq) and methylisothiocyanate polystyrene resin (4 eq) are added to the mixture diluted in dichloromethane. After stirring for 6 hours at approximately 20° C., the mixture is filtered and the filtrate is concentrated under reduced pressure at 40° C. in order to produce the expected compound in the form of an oil (27 mg, 90% yield).

1. stirringAfter stirring for 15 hours at approximately 20° C.
2. stirringAfter stirring for 6 hours at approximately 20° C.
3. filtrationthe mixture is filtered
4. concentrationthe filtrate is concentrated under reduced pressure at 40° C. in order