化学合成。
医药
合成路线 1(1. 合成:139755-99-0)
产率:98%
合成条件:With hydrogenchloride In water at 100℃;
实验步骤:将I-03a(11g,56.12mmol)在HCl(121mL,6M)中的溶液加热至100℃过夜。 将反应混合物真空浓缩,用EA萃取,用水洗涤,将有机层真空浓缩,得到I-04a(9.4g,收率98%)。 ESI-MS(Mi-i):169计算值。 对于08H12N202:168.1。
参考文献:
- [1] Patent: WO2014/131855, 2014, A1. Location in patent: Page/Page column 80 [2] Patent: WO2016/20307, 2016, A1. Location in patent: Page/Page column 50 [3] Patent: US2008/194529, 2008, A1. Location in patent: Page/Page column 56-57 [4] Patent: WO2015/114647, 2015, A1. Location in patent: Page/Page column 46; 47 [5] Patent: US5250534, 1993, A [6] Patent: US5272147, 1993, A [7] Patent: US6200980, 2001, B1 [8] Patent: US6200980, 2001, B1 [9] Bioorganic and Medicinal Chemistry Letters, 1996, vol. 6, # 15, p. 1819 - 1824 [10] Bioorganic and Medicinal Chemistry Letters, 2005, vol. 15, # 17, p. 3900 - 3907 [11] European Journal of Medicinal Chemistry, 2015, vol. 90, p. 889 - 896