反应详情

BMS (0.015 mL, 0.15 mmol) was added to a solution of 2-(propylamino)-N-(5-(4-p-tolylthiazol-2-ylcarbamoyl)thiazol-2-yl)thiazole-5-carboxamide (15 mg, 0.03 mmol) in THF (1 mL) at RT. The resulting solution was stirred at RT overnight. The reaction was then quenched with MeOH (0.5 mL). 1N HCl was added until pH=2. After stirring the reaction mixture at RT for 12 hrs, the organic solvents were evaporated and the aqueous solution was neutralized with a NaHCO3 saturated aqueous solution, extracted with AcOEt, dried with Na2SO4 and concentrated. The crude product was purified by column chromatography (0%-5% MeOH/AcOEt), yielding N-propyl-5-((5-((4-p-tolylthiazol-2-ylamino)methyl)thiazol-2-ylamino)methyl)thiazol-2-amine (5 mg, 32%).

1. customThe reaction was then quenched with MeOH (0.5 mL)
2. addition1N HCl was added until pH=2
3. stirringAfter stirring the reaction mixture at RT for 12 hrs
4. customthe organic solvents were evaporated
5. extractionextracted with AcOEt
6. dry with materialdried with Na2SO4
7. concentrationconcentrated
8. customThe crude product was purified by column chromatography (0%-5% MeOH/AcOEt)