(S)-2-羟基-3-甲氧基-3,3-二苯基丙酸主要作为医药中间体或原料药,用于相关药物的合成制备。
医药
路线1:
- 步骤:将500mg(1.84mmol)的(RS)-2-羟基-3-甲氧基-3,3-二苯基丙酸溶于8mL的2-丙醇中,加入135mg(0.92mmol)的(S)-(+)-1,2,3,4-四氢-1-萘胺,加热回流搅拌1小时后冷却至室温并搅拌2小时,过滤收集沉淀晶体,用2-丙醇洗涤,减压干燥。
- 条件:With (S)-1,2,3,4-tetrahydronapht-1-yl-amine In tert-butyl methyl ether for 1 h; Reflux
- 收率:89%
- 参考文献:[1] Patent: JP2017/128528, 2017, A. Location in patent: Paragraph 0005; 0041; 0042; 0045; 0046 [2] Patent: WO2012/17441, 2012, A1. Location in patent: Page/Page column 11-12 [3] Patent: CN104098462, 2017, B. Location in patent: Paragraph 0009; 0028; 0029; 0031 [4] Patent: JP5700378, 2015, B2. Location in patent: Paragraph 0071; 0072 [5] Patent: WO2013/57468, 2013, A1. Location in patent: Page/Page column 23-24 [6] Journal of Medicinal Chemistry, 1999, vol. 42, # 16, p. 3026 - 3032 [7] Patent: WO2010/70658, 2010, A2. Location in patent: Page/Page column 19 [8] Patent: US2011/263854, 2011, A1. Location in patent: Page/Page column 10 [9] Patent: US2011/263854, 2011, A1. Location in patent: Page/Page column 8 [10] Patent: WO2014/1511, 2014, A1 [11] Patent: WO2014/1511, 2014, A1 [12] Patent: KR2016/39907, 2016, A
路线2:
- 步骤:向装有含有形式I(98%ee)(200mg,0.30mmol)的圆底烧瓶中加入水/TBME(1:1)(10mL)的混合物,室温搅拌30分钟,相分离后分离水相,用TBME(3×5mL)萃取,合并有机萃取液用水(10mL)洗涤,干燥(MgSO₄)并真空蒸馏。