反应详情

100 mg (0.37 mmol) of 1-(4-bromothiazol-2-yl)piperidin-4-one from step a and 22 μl (0.37 mmol) of 2-aminoethanol were suspended in 7 ml of THF, stirred at room temperature for 1 h, 21 μl (0.37 mmol) of glacial acetic acid and 164 mg (0.74 mmol) of sodium triacetoxyborohydride were added. The mixture was stirred at room temperature overnight, water and EA were added, the mixture was adjusted to pH 12 using a concentrated NaOH solution and extracted by shaking with EA. The organic phase was dried over sodium sulfate, filtered and evaporated.

1. stirringThe mixture was stirred at room temperature overnight
2. extractionextracted
3. stirringby shaking with EA
4. dry with materialThe organic phase was dried over sodium sulfate
5. filtrationfiltered
6. customevaporated