252723-17-4
252723-17-4 结构式
基本信息
5-broMo-4-chloro-7-(phenylsulfonyl)-7H-pyrrolo[2,3-d]pyriMidine
7H-Pyrrolo[2,3-d]pyrimidine, 5-bromo-4-chloro-7-(phenylsulfonyl)-
物理化学性质
制备方法
22276-95-5
98-09-9
252723-17-4
在0℃下,将5-溴-4-氯-7H-吡咯并[2,3-d]嘧啶(3.0g,13mmol)溶于DMF(40mL)中,缓慢加入NaH(60%w/w于矿物油中,720mg,18.1mmol)。在氮气保护下,于0℃搅拌反应混合物30分钟。随后,滴加苯磺酰氯(1.7g,13mmol),将反应混合物升温至室温并继续搅拌2小时。反应完成后,加入水(200mL)以诱导沉淀。通过过滤收集沉淀物,并真空干燥,得到白色固体7-苯磺酰基-5-溴-4-氯-7H-吡咯并[2,3-d]嘧啶(4.9g,收率100%)。产物经1H NMR(DMSO-d6, 400MHz)表征:δ 8.85(1H, s),8.45(1H, s),8.19(2H, d, J=8.7Hz),7.81(1H, t, J=7.4Hz),7.70(2H, t, J=7.8Hz)。
参考文献:
[1] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 19, p. 5607 - 5612
[2] Patent: WO2005/51304, 2005, A2. Location in patent: Page/Page column 117
[3] Patent: WO2005/51304, 2005, A2. Location in patent: Page/Page column 117
[4] Patent: US6635762, 2003, B1. Location in patent: Page/Page column 26
[5] Patent: US2009/42893, 2009, A1. Location in patent: Page/Page column 14