反应详情

Preparation of 7-(4-bromo-2-fluorophenylamino)-imidazo[1,2-b]pyridazine-6-carboxylic acid (2-vinyloxyethoxy)-amide: A mixture of 7-(4-bromo-2-fluorophenylamino)-imidazo[1,2-b]pyridazine-6-carboxylic acid (1.00 equiv), EDCI (1.50 equivalents), and HOBt (1.50 equivalents) in DMA is stirred for 30 minutes at room temperature under N2. O-(2-vinyloxy-ethyl)-hydroxylamine (3.00 equivalents) is added followed by Et3N (2.50 equivalents). After the reaction mixture is stirred for 16 hours at room temperature, it is diluted with EtOAc and washed with saturated NH4Cl solution, saturated NaHCO3 solution and saturated NaCl. The organic layer is dried (Na2SO4) and concentrated under reduced pressure to yield the desired product. The product may be purified by flash column chromatography if further purification is necessary.

1. stirringAfter the reaction mixture is stirred for 16 hours at room temperature
2. washwashed with saturated NH4Cl solution, saturated NaHCO3 solution and saturated NaCl
3. dry with materialThe organic layer is dried (Na2SO4)
4. concentrationconcentrated under reduced pressure