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-bromobenzyl)thio]-1-{3-[methyl(2-pyridin-2-ylethyl)amino]propyl}-1H-benzimidazole-5-carboxylic acid (27 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 4-(1-pyrrolidinyl)piperidine (15 mg, 2 eq) is added. After stirring for 15 hours at approximately 20° C., aminomethyl polystyrene resin (2 eq, acquired from Novabiochem), TBD-methyl polystyrene resin (2 eq, acquired from Novabiochem) and methylisothiocyanate polystyrene resin (4 eq, acquired from Novabiochem) 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 (28 mg, 84% 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