反应详情

A solution of 5-(4-fluorophenoxy)-1-isobutyl-1H-indazole-6-carboxylic acid (compound 10g, prepared as described in Example 46) in THF was treated with carbonyldiimidazole (1.2 equivalents) at room temperature under nitrogen atmosphere. After stirring for 18 hours, the reaction was treated with N1-Methyl-N1-phenyl-propane-1,3-diamine (1 equivalent). After 18 additional hours, the solvent was allowed to slowly evaporate and the residue was purified in a Sep Pak cartridge eluting with a gradient of 100% CH2Cl2 to 5% MeOH/CH2Cl2 to provide compound 11g-12 as an oil in 78% yield.

1. customto slowly evaporate
2. customthe residue was purified in a Sep Pak cartridge
3. washeluting with a gradient of 100% CH2Cl2 to 5% MeOH/CH2Cl2
4. customto provide compound 11g-12 as an oil in 78% yield