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：
- [1] Patent: WO2008/23161, 2008, A1. Location in patent: Page/Page column 121-122 [2] Patent: WO2016/161145, 2016, A1. Location in patent: Paragraph 00746 [3] Patent: WO2016/180536, 2016, A1. Location in patent: Page/Page column 199 [4] Patent: US2009/286798, 2009, A1. Location in patent: Page/Page column 28-29 [5] Patent: WO2007/131991, 2007, A1. Location in patent: Page/Page column 91 [6] Patent: WO2007/138072, 2007, A2. Location in patent: Page/Page column 82-83 [7] Patent: WO2011/134468, 2011, A1. Location in patent: Page/Page column 132 [8] Patent: WO2008/51493, 2008, A2. Location in patent: Page/Page column 140 [9] Patent: WO2005/73205, 2005, A1. Location in patent: Page/Page column 25 [10] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 3, p. 1293 - 1297 [11] Patent: WO2013/41497, 2013, A1. Location in patent: Page/Page column 39; 40 [12] Patent: US2013/172327, 2013, A1. Location in patent: Paragraph 0200; 0201 [13] Patent: WO2013/148603, 2013, A1. Location in patent: Paragraph 0230-0231 [14] Patent: WO2014/90692, 2014, A1. Location in patent: Page/Page column 63 [15] Patent: WO2008/65199, 2008, A1. Location in patent: Page/Page column 75
