反应详情

DIPEA (51 mg; 0.392 mmol) is added to a suspension of 1-methyl-6-oxo-1,6-dihydro-pyridine-3-carboxylic acid D-7 (20 mg; 0.131 mmol) and HATU (70 mg; 0.183 mg) in DMF. The mixture is stirred at RT for 5 min. N2-Benzyl-6-(4-methyl-piperazin-1-yl)-pyridine-2,3-diamine E-3.1 is then added and the reaction mixture stirred at RT for 1 h. The reaction mixture is extracted with DCM and NaHCO3 solution. The organic layer is dried over Na2SO4 and concentrated in vacuum. To the formed amide is added 1 ml glacial acetic acid, the reaction is stirred at 120° C. for 2 days. The crude reaction mixture is purified by using reversed phase chromatography (Method: prep. HPLC1).

1. stirringthe reaction mixture stirred at RT for 1 h
2. extractionThe reaction mixture is extracted with DCM and NaHCO3 solution
3. dry with materialThe organic layer is dried over Na2SO4
4. concentrationconcentrated in vacuum
5. additionTo the formed amide is added 1 ml glacial acetic acid
6. stirringthe reaction is stirred at 120° C. for 2 days
7. customThe crude reaction mixture
8. customis purified