反应详情

3,4 dimethoxyphenylisothiocyanate (35 mg, 1.2 eq) and N-methylcyclohexylcarbodiimide-N-methyl-polystyrene resin (acquired from Novabiochem; charge 1.69 mmol/g, 355 mg, 4 eq) are added successively to a solution of 3-amino-4-({3-[benzyl(methyl)amino]propyl}amino)-N,N-diisobutylbenzamide (65 mg, 1 eq) in tetrahydrofuran (2 ml). The mixture is heated under reflux for 18 hours then cooled down to ambient temperature and aminomethyl polystyrene resin (acquired from Novabiochem, 2 eq) is added. After stirring for 4 hours at ambient temperature, the mixture is filtered on frit and the filtrate is concentrated under reduced pressure at 40° C. The residue obtained is dissolved in ethyl ether and a 1N solution of HCl in ethyl ether is added dropwise in order to produce the expected compound in the form of the hydrochloride salt (81 mg, 92% yield).

1. temperatureThe mixture is heated
2. temperatureunder reflux for 18 hours
3. filtrationthe mixture is filtered on frit
4. concentrationthe filtrate is concentrated under reduced pressure at 40° C
5. customThe residue obtained