反应详情

The compound (171.8 mg) obtained in Example 112-2 was dissolved in anhydrous methanol (7.0 ml). The solution was added with 1-methyl-2-imidazole carboxaldehyde (65.0 mg) and sodium cyanoborohydride (49.0 mg). Then, the solution was adjusted to pH 5 with acetic acid and then stirred at room temperature for 2 days. After the reaction, the solvent was distilled off. The residue was added with a 1 mol/l sodium hydroxide aqueous solution and extracted with chloroform. The extract was dried with magnesium sulfate, and the solvent was distilled off. Then, the residue was purified through silica gel column chromatography (chloroform/methanol) and treated with hydrochloric acid, thereby obtaining hydrochloride (184.8 mg) of the subject compound as a white solid.

1. customAfter the reaction
2. distillationthe solvent was distilled off
3. additionThe residue was added with a 1 mol/l sodium hydroxide aqueous solution
4. extractionextracted with chloroform
5. dry with materialThe extract was dried with magnesium sulfate
6. distillationthe solvent was distilled off
7. customThen, the residue was purified through silica gel column chromatography (chloroform/methanol)
8. additiontreated with hydrochloric acid