反应详情

The coupling of 4-(7-bromo-1-oxo-1H-3,5,8-triazaisoquinolin-2-ylmethyl)benzoic acid tert-butyl ester (0.70 g, 1.69 mmol) with 1-prop-2-ynyl-1H-imidazole (0.45 g, 4.22 mmol) using triethylamine (0.94 mL, 6.76 mmol), CuI (0.023 g, 0.12 mmol), and Pd(Ph3P)4 (0.08 g, 0.07 mmol) in dimethyl-formamide is carried out as described in Example 1, Step (2). The silica gel mesh is purified on a 3.5×18 cm silica gel column eluted with hexanes/ethyl acetate 1:1, methylene chloride/THF 7:1, then methylene chloride/THF 4:1. Evaporation and drying will afford the desired product.

1. customThe silica gel mesh is purified on a 3.5×18 cm silica gel column
2. washeluted with hexanes/ethyl acetate 1:1, methylene chloride/THF 7:1
3. customEvaporation
4. customdrying will