反应详情

45.4 mg (0.30 mmol) of 3-methoxyphenyl isocyanate and 84.8 μl (0.61 mmol) of triethylamine are added to a solution of 60 mg (0.15 mmol) of ((3R)—N-(4′-aminobiphenyl-4-yl)quinuclidine-3-carboxamide dihydrochloride (Example 7A) in 0.5 ml of DMF. After 18 h at room temperature, 5 ml of water are added to the reaction mixture. The resulting precipitate is filtered off with suction, washed with water and dried under high vacuum. A preparative HPLC is carried out for further purification. The product fractions are concentrated, mixed with 3 ml of 1 N hydrochloric acid, again concentrated and dried under high vacuum. 22 mg (27.6% of theory) of the title compound are obtained.

1. filtrationThe resulting precipitate is filtered off with suction
2. washwashed with water
3. customdried under high vacuum
4. customA preparative HPLC is carried out for further purification
5. concentrationThe product fractions are concentrated
6. additionmixed with 3 ml of 1 N hydrochloric acid
7. concentrationagain concentrated
8. customdried under high vacuum