作为医药中间体,用于相关药物合成研究。
医药中间体
合成路线 1(1. 合成:335255-43-1)
产率:100%
合成条件:With palladium 10% on activated carbon; hydrogen In methanol at 20℃; for 2 h;
实验步骤:通用方法:(2-氨基-4-(噻吩-2-基)苯基)氨基甲酸叔丁酯(9a)的合成:按照专利文献(WO2009 / 055917)中报道的方法制备化合物9a。 将化合物8a(0.24g,0.75mmol)置于圆底烧瓶中,并向其中加入10%碳载钯(催化量,20mg)。 将反应混合物暴露于气球。 用反应混合物吹扫后,在室温下在气球下搅拌2小时。 然后将其通过Ceiite过滤并在真空下浓缩,得到所需的胺(0.217g,100%收率).1E NMR(400MHz,氯仿-d)δ7.33-7.27(m,1H),7.25-7.21(m,2H) )57.08-7.03(m,2H),7.02(d,J = 2.0Hz,1H),1.52(s,9H)。
参考文献:
- [1] Patent: WO2014/160221, 2014, A1. Location in patent: Page/Page column 49 [2] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 12, p. 2981 - 2994 [3] Patent: WO2007/118137, 2007, A1. Location in patent: Page/Page column 83 [4] European Journal of Medicinal Chemistry, 2017, vol. 134, p. 185 - 206 [5] Patent: US9365498, 2016, B2. Location in patent: Page/Page column 121 [6] ACS Medicinal Chemistry Letters, 2014, vol. 5, # 4, p. 340 - 345 [7] Patent: US9365498, 2016, B2. Location in patent: Page/Page column 120; 121 [8] European Journal of Medicinal Chemistry, 2015, vol. 96, p. 340 - 359 [9] Patent: US6509328, 2003, B1 [10] Patent: US2007/117824, 2007, A1. Location in patent: Page/Page column 28-29 [11] Bioorganic and Medicinal Chemistry Letters, 2008, vol. 18, # 2, p. 726 - 731 [12] Patent: WO2007/136605, 2007, A2. Location in patent: Page/Page column 51