Synthesis
4-Chloro-1H-pyrazolo[3,4-d]pyrimidine (1.1 g, 7.1 mmol) was used as starting material and suspended in CHCl3 (50 mL). N-bromosuccinimide (NBS, 1.49 g, 8.4 mmol) was added to the suspension under stirring. The reaction mixture was stirred at room temperature for 5 h and subsequently cooled to 0°C. The resulting solid product was separated by vacuum filtration and washed with cold CHCl3. The solid product was dried over air and further purified by silica gel column chromatography (eluent: 50% EtOAc/hexanes) to afford finally 3-bromo-4-chloro-1H-pyrazolo[3,4-d]pyrimidine (1.3 g, 77% yield).
References
[1] Organic Letters, 2003, vol. 5, # 20, p. 3587 - 3590
[2] Patent: WO2005/51304, 2005, A2. Location in patent: Page/Page column 115-116
[3] Patent: WO2005/51304, 2005, A2. Location in patent: Page/Page column 115-116
[4] MedChemComm, 2018, vol. 9, # 8, p. 1340 - 1350
[5] Patent: WO2016/187723, 2016, A1. Location in patent: Page/Page column 51