反应详情

To a suspension of (2S)-3-((6-chloronaphthalen-2-yl)sulfonyl)-2-hydroxypropanoic acid (0.32 g), N-((2Z)-3-methyl-4-(-1-piperazinylmethyl)-1,3-thiazol-2(3H)-ylidene)methanamine trihydrochloride (0.51 g), HOBt (0.20 g) and triethylamine (0.63 mL) in DMF (5 mL), WSC (0.21 g) was added, and the mixture was mixed at room temperature for 22 hours. The reaction solution was concentrated under reduced pressure. The residue was basified with an aqueous potassium carbonate solution, and then the mixture was extracted with ethyl acetate/THF. The extract was dried over anhydrous magnesium sulfate, the solvent was then distilled off, and the residue was purified with a basic silica gel column to give the title compound (0.12 g, 23%) as a colorless powder.

1. additionwas added
2. additionthe mixture was mixed at room temperature for 22 hours
3. concentrationThe reaction solution was concentrated under reduced pressure
4. extractionthe mixture was extracted with ethyl acetate/THF
5. dry with materialThe extract was dried over anhydrous magnesium sulfate
6. distillationthe solvent was then distilled off
7. customthe residue was purified with a basic silica gel column