反应详情

3-Bromo-5-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine (300 mg, 1.1 mmol) taken up in 10 mL DMF. Boc-Ser(Me)-OH (280 mg, 1.3 mmol), HATU (368 mg, 1.6 mmol), and triethylamine (590 uL, 4.25 mmol) was added and stirred at room temp overnight. Reaction was diluted with DCM and washed with water. DCM layer was dried over magnesium sulfate reduced in vacuo. This was then taken up in 30% TFA in DCM solution and stirred at room temperature for 2 hours. It was then cooled to 0° C. and conc Aq NaOH added slowly until aqueous layer remains basic. DCM layer extracted dried over magnesium sulfate, reduced in vacuo for 405 mg crude product for further reaction as is. LRMS (ESI) m/z 383/385 [(M+H)]+, calc'd for C14H19BrN6O2: 383.25.

1. customReaction
2. washwashed with water
3. dry with materialDCM layer was dried over magnesium sulfate
4. stirringstirred at room temperature for 2 hours
5. temperatureIt was then cooled to 0° C.
6. additionconc Aq NaOH added slowly until aqueous layer
7. extractionDCM layer extracted
8. dry with materialdried over magnesium sulfate
9. customreduced in vacuo for 405 mg crude product for further reaction