4752-10-7 1,4-二氯酞嗪

运输信息：常温运输。危险描述：非危险化学品，WGK Germany:3，海关编码29339900，存储类别11 - 可燃固体。

化学合成，医药中间体；白色结晶，熔点160-162℃，用作医药中间体。

医药

合成路线 1（1. 合成：4752-10-7）

• 步骤：将化合物1（1.68g，10mmol）加入搅拌的磷酰氯（15ml）溶液中，加热至110℃并保持1小时，反应完成后（通过TLC监测），将反应混合物冷却至室温，滴加到碎冰中并搅拌10分钟，通过布氏漏斗过滤，滤饼用H₂O洗涤至中性并在真空中干燥，得到产物2（1.85g，90.1％），为白色固体。
• 条件：110℃，1小时；TLC监测反应完成。
• 产率：90.1%。
• 参考文献：[1] Bioorganic and Medicinal Chemistry Letters, 2014, vol. 24, #4, p.1236-1238；[2] European Journal of Medicinal Chemistry, 2014, vol.85, p.235-244；[3] Chemical Biology and Drug Design, 2013, vol.81, #5, p.591-599；[4] New Journal of Chemistry, 2016, vol.40, #7, p.6070-6076；[5] Bioorganic and Medicinal Chemistry Letters, 2016, vol.26, #6, p.1576-1579；[6] Journal of Natural Products, 2009, vol.72, #11, p.2072-2075；[7] European Journal of Medicinal Chemistry, 2010, vol.45, #11, p.4807-4812；[8] Asian Journal of Chemistry, 2011, vol.23, #1, p.127-131；[9] Organic Process Research and Development, 2011, vol.15, #5, p.1149-1162；[10] Bioorganic and Medicinal Chemistry Letters, 2013, vol.23, #7, p.2007-2013；[11] Journal of Organic Chemistry, 1993, vol.58, #4, p.844-849；[12] Patent: WO2006/74223, 2006, A2. Location in patent: Page/Page column 59；[13] Patent: EP2799435, 2014, A1. Location in patent: Paragraph 0050; 0072; 0073；[14] Patent: US2015/51211, 2015, A1. Location in patent: Paragraph 0098; 0099；[15] Journal of the Chemical Society, 1937, p.16,25；[16] Journal of the Indian Chemical Society, 1990, vol.67, #9, p.779-780；[17] Arzneimittel-Forschung/Drug Research, 2010, vol.60, #6, p.289-292；[18] Letters in Drug Design and Discovery, 2012, vol.9, #4, p.409-414；[19] Journal of Enzyme Inhibition and Medicinal Chemistry, 2013, vol.28, #4, p.792-800；[20] Bioorganic and Medicinal Chemistry Letters, 2014, vol.24, #7, p.1737-1741；[21] Patent: US2015/374705, 2015, A1. Location in patent: Paragraph 0289; 0290；[22] Patent: CN104016986, 2016, B. Location in patent: Paragraph 0037；[23] Patent: CN103694244, 2016, B. Location in patent: Paragraph 0044；[24] Archiv der Pharmazie, 2017, vol.350, #12；[12] Patent: WO2006/74223, 2006, A2. Location in patent: Page/Page column 59；[13] Patent: EP2799435, 2014, A1. Location in patent: Paragraph 0050; 0072; 0073；[14] Patent: US2015/51211, 2015, A1. Location in patent: Paragraph 0098; 0099；[21] Patent: US2015/374705, 2015, A1. Location in patent: Paragraph 0289; 0290；[22] Patent: CN104016986, 2016, B. Location in patent: Paragraph 0037；[23] Patent: CN103694244, 2016, B. Location in patent: Paragraph 0044；

合成路线 2（由苯酐经环合、氯化而得）

• 步骤：苯酐经环合、氯化反应得到1,4-二氯酞嗪。