反应详情

5-(2-Aminopyridin-4-ylamino)indole-1-carboxylic acid phenylamide (69 mg, 0.20 mmol, Production example 201-3) was dissolved in tetrahydrofuran (14 ml); triethylamine (0.055 ml, 0.40 mmol) was added thereto; and phenyl chloroformate (0.038 ml, 0.30 mmol) was added while stirring and cooled by ice. A portion of 7.0 ml of this reaction mixture was transferred to another vessel; and the remaining portion of the reaction mixture was concentrated under reduced pressure. The residue was dissolved in N,N-dimethylformamide (1.0 ml); the similar reaction to Example 201 was performed using N,N-diethyl-1,3-diaminopropane (0.047 ml, 0.30 mmol); the crude product obtained was purified by a TLC plate (Fuji Silysia NH, developing solvent:ethyl acetate/ethanol=10/1); and the obtained crystals were suspended in ethyl acetate, filtered off, and dried to yield the title compound (3 mg, 0.006 mmol) as colorless crystals.

1. temperaturecooled by ice
2. concentrationand the remaining portion of the reaction mixture was concentrated under reduced pressure
3. dissolutionThe residue was dissolved in N,N-dimethylformamide (1.0 ml)
4. customthe similar reaction to Example 201
5. customthe crude product obtained
6. customwas purified by a TLC plate (Fuji Silysia NH, developing solvent:ethyl acetate/ethanol=10/1)
7. filtrationfiltered off
8. customdried