4-(4-Boc-1-piperazinyl)-5-bromo-7H-pyrrolo[2,3-d]pyrimidine is used as a reactant in the preparation of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives as Akt inhibitors with antiproliferative effects.
5-Bromo-4-chloro-7H-pyrrolo[2,3-d]pyrimidine (5 mmol) and N-BOC-piperazine (6 mmol) were dissolved in 5 mL of dioxane in the presence of diisopropylethylamine (DIEA, 7.5 mmol). The reaction mixture was placed in a microwave reactor and heated at 80 °C for 2 hours. After completion of the reaction, the solvent was removed by distillation under reduced pressure. The crude product obtained was purified by recrystallization to afford intermediate 3, 4-(4-BOC-1-piperazinyl)-5-bromo-7H-pyrrolo[2,3-d]pyrimidine, as a white solid in 78.5% yield.
[1] Patent: CN108997351, 2018, A. Location in patent: Paragraph 0075; 0112; 0151; 0152
[2] Archiv der Pharmazie, 2016, vol. 349, # 5, p. 356 - 362
[3] European Journal of Medicinal Chemistry, 2017, vol. 138, p. 543 - 551
[4] Patent: WO2008/128072, 2008, A2. Location in patent: Page/Page column 39; 40
![4-(4-Boc-1-piperazinyl)-5-broMo-7H-pyrrolo[2,3-d]pyriMidine Structure](/CAS/GIF/1072027-36-1.gif)
![5-Bromo-4-chloro-7H-pyrrolo[2,3-d]pyrimidine](/CAS/GIF/22276-95-5.gif)
