反应详情

To 2.0 g. of the 5-(2-aminomethylprop-2-yl)-2-(4-pyridinyl)-benzimidazole (prepared in Example 1) and 830 mg. triethylamine in 50 ml. dry dichloromethane are added dropwise, while cooling with ice water, 953 mg. mesyl chloride. The reaction mixture is stirred for 10 minutes and then 20 ml. water are added thereto. After filtering off with suction, washing with water and dichloromethane and recrystallising from water/ethanol (2:1 v/v), there are obtained 2.0 g. (85% of theory) of the title compound as a hydrate in the form of yellowish crystals which sinter above 130° C., again crystalline above 150° C. and then melt at 215°-216° C.

1. filtrationAfter filtering off with suction
2. washwashing with water and dichloromethane
3. customrecrystallising from water/ethanol (2:1 v/v), there
4. customare obtained 2.0 g