376584-62-2 1-异吲哚酮-5-硼酸频哪醇酯

危险性质：非危险化学品

化学合成。

医药

合成路线 1（1. 合成：376584-62-2）

产率：94% 合成条件：With potassium acetate In 1,4-dioxane at 70 - 120℃; for 18 h; 实验步骤：向5-溴-2,3-二氢 - 异吲哚-1-酮（1当量）的无水二恶烷（0.1M）溶液中加入双（频哪醇）二硼（1.1当量），乙酸钾（3.5当量）和dppf。 （0.05当量）。将反应混合物用氮气脱气20分钟。将PdCl 2（dppf）（0.05当量）加入到反应混合物中，将其再脱气5分钟。将反应混合物在氮气下加热至70℃并保持2小时，然后加热至120℃保持16小时。将反应混合物在EtOAc和水之间分配。将水相进一步用EtOAc萃取，将合并的有机相干燥（MgSO 4），过滤并真空浓缩。将残余物溶解在CH 2 Cl 2中并加入己烷。过滤得到的悬浮液，干燥收集的棕色粉末，无需进一步纯化即可使用.5-（4,4,5,5-四甲基 - [1,3,2]二氧杂硼杂环戊烷-2-基）-2,3-二氢-isoindol-l-one：（产率94％，纯度76％，主要杂质为硼酸13％）m / z（LC-MS，ESP）：260.4 [2M + H] + R / T = 3.51min 参考文献：

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