反应详情

3-bromo-5-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine (400 mg, 1.42 mmol) Boc-L-Leucine (392 mg, 1.7 mmol), HATU (490 mg, 2.13 mmol), and triethylamine (788 uL, 5.7 mmol) taken up in DMF and stirred at room temperature overnight. Reaction diluted with DCM washed with water, DCM layer then dried over magnesium sulfate filtered and reduced in Vacuo. This was then taken up in 26 mL DCM and 4 mL TFA added. Stirred 1 hour until complete by LC/MS. Reaction was washed with 1N NaOH, DCM layer removed dried over magnesium sulfate filtered, reduced in vacuo to obtain 349 mg crude product for further reaction as is. LRMS (ESI) m/z 381/383 [(M+H)]+, calc'd for C15H21BrN6O: 381.28.

1. customReaction
2. washwashed with water, DCM layer
3. dry with materialthen dried over magnesium sulfate
4. filtrationfiltered
5. addition4 mL TFA added
6. stirringStirred 1 hour until complete by LC/MS
7. customReaction
8. washwas washed with 1N NaOH, DCM layer
9. customremoved
10. dry with materialdried over magnesium sulfate
11. filtrationfiltered