Methyl p-toluenesulfonate → 4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(2-(7-methoxy-5-azaspiro[2.4]heptan-5-yl)ethoxy)quinoline

Participants

Reaction Conditions

Reaction Steps

The above product from Example 2 (60 mg) was dissolved into DMF (4 ml) and cooled at 0° C. NaH (1.1 eq) was added to the reaction and stirred for 10 minutes. To the reaction was added TsOMe (1.2 eq), the solution was heated at 80° C. for two hours. The reaction was quenched with water and extracted with EtOAc followed by washing with water, then brine and dried over Na2SO4. The solution was evaporated and purified by silica column to give the titled product. Mass: (M+1), 492

Provenance & Evidence