6-溴-3,4-二氢-2H-异喹啉-1-酮可用作医药合成中间体。
医药
路线1：
- 步骤: 在0℃下，将甲磺酸加入到溴茚酮在二氯甲烷中的混合物中，分批加入叠氮化钠，加完后搅拌30分钟；加入NaOH的含水混合物直至微碱性，二氯甲烷萃取，减压蒸发有机层，硅胶柱色谱纯化（0至50％EtOAc/己烷，然后0至7％MeOH/CH₂Cl₂）得到产物。
- 条件: Stage #1: 0℃，二氯甲烷，甲磺酸，叠氮化钠；Stage #2: 二氯甲烷，水，NaOH；
- 收率: 61%
- 参考文献: [1] Patent: US2010/4231, 2010, A1. Location in patent: Page/Page column 67-68 [2] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 9, p. 2670 - 2674 [3] Patent: US2016/251376, 2016, A1. Location in patent: Paragraph 0852; 0853; 0854 [4] Patent: EP3239143, 2017, A2. Location in patent: Paragraph 0088 [5] Patent: CN107879975, 2018, A. Location in patent: Paragraph 0132; 0134 [6] Patent: WO2011/51490, 2011, A2. Location in patent: Page/Page column 22 [7] Patent: US2009/69300, 2009, A1. Location in patent: Page/Page column 14 [8] Patent: CN106565674, 2017, A. Location in patent: Paragraph 0283; 0284; 0285; 0286; 0287 [9] Patent: WO2018/160406, 2018, A1. Location in patent: Page/Page column 10 [10] Patent: WO2006/21805, 2006, A1. Location in patent: Page/Page column 75 [11] Patent: WO2009/98144, 2009, A1. Location in patent: Page/Page column 75 [12] Patent: WO2004/65351, 2004, A1. Location in patent: Page 110 [13] Patent: US2010/222325, 2010, A1. Location in patent: Page/Page column 98; 107 [14] Patent: EP1724263, 2006, A1. Location in patent: Page/Page column 40 [15] Journal of Medicinal Chemistry, 2012, vol. 55, # 5, p. 2452 - 2468 [16] Patent: US2018/51013, 2018, A1. Location in patent: Paragraph 0597; 0598; 0629; 0630
路线2：
- 步骤: 将6-溴-3,4-二氢异喹啉-1（2H）-酮加入到5-溴-1-茚满酮在二氯甲烷和甲烷磺酸（1:1）的混合物中，分批加入叠氮化钠，室温搅拌8小时；冷却至0℃，用5% NaOH水溶液中和，乙酸乙酯萃取，合并有机层洗涤、干燥、浓缩，硅胶柱色谱纯化（30%乙酸乙酯的己烷溶液）得到产物。
- 条件: Stage #1: 0-20℃，二氯甲烷，甲烷磺酸，叠氮化钠；Stage #2: 0℃，二氯甲烷，水，NaOH；
- 收率: 60%
- 参考文献: [1] Patent: WO2012/162129, 2012, A1. Location in patent: Page/Page column 35 [2] Patent: US2015/307445, 2015, A1. Location in patent: Paragraph 0441; 0442; 0443 [3] Patent: US2006/63799, 2006, A1. Location in patent: Page/Page column 9
路线3：
- 步骤: 在0℃下，向2-（（苄基氨基甲酰基）氧基）苯甲酸甲酯的无水二氯甲烷溶液中加入三氟甲磺酸，20℃和氩气氛下搅拌1小时；冰水淬灭，二氯甲烷萃取，硫酸钠干燥，柱色谱纯化（乙酸乙酯：氯仿=1:2）得到产物。
- 条件: 0-20℃，二氯甲烷，三氟甲磺酸，氩气；
- 收率: 56%
- 参考文献: [1] Heterocycles, 2016, vol. 93, # 2, p. 705 - 713
路线4：
- 步骤: 称取5-溴-1-茚满酮置于圆底烧瓶中，依次加入二氯甲烷、甲磺酸和叠氮化钠，室温搅拌反应3小时；反应完成后，加入1.0 M氢氧化钠水溶液淬灭，二氯甲烷萃取，合并有机相，饱和盐水洗涤，无水硫酸钠干燥，减压浓缩，硅胶柱色谱纯化（石油醚/乙酸乙酯=3:1）得到产物。
- 条件: 0℃，二氯甲烷，甲磺酸，叠氮化钠；室温搅拌3小时；
- 收率: 39%
- 参考文献: [1] Patent: US2010/4231, 2010, A1. Location in patent: Page/Page column 67-68 [2] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 9, p. 2670 - 2674 [3] Patent: US2016/251376, 2016, A1. Location in patent: Paragraph 0852; 0853; 0854
