3-[(1R)-3-[二(1-甲基乙基)氨基]-1-苯基丙基]-4-(苯基甲氧基)-苯甲酸盐酸盐合成路线 (共 15 条)
反应条件
1.1: sodium hydroxide / water 2.1: ethyl bromide; iodine; magnesium / tetrahydrofuran / 1 h / 55 °C / Reflux 2.2: 1 h / -65 - -60 °C View Scheme
参考文献
ACTAVIS GROUP PTC EHF
Patent: US2011/124903 A1, 2011 ;
反应条件
1: thionyl chloride / 5 h / 40 - 45 °C 2: hydrogen / 5 palladium on charcoal / ethyl acetate / 18 h / 25 - 30 °C / 2206.72 - 2942.29 Torr / autoclave 3: diisobutylaluminium hydride / toluene / 1 h / -78 °C / Inert atmosphere 4: hydrogen / 5 palladium on charcoal / methanol / 8 h / 25 - 30 °C / 2206.72 - 2942.29 Torr / autoclave View Scheme
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; THIRUMALAI RAJAN, Srinivasan; ESWARAIAH, Sajja; RAGHURAM, Suraparaju; SEETHA RAMA SARMA, Peri
Patent: WO2012/98560 A2, 2012 ;
WO 2012/098560 A2
反应条件
1: thionyl chloride / 10 °C / Reflux 2: lithium aluminium tetrahydride / tetrahydrofuran / 14 h / 25 - 30 °C 3: hydrogen / 5 Pd(II)/C(eggshell) / methanol / 50 - 55 °C View Scheme
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; THIRUMALAI RAJAN, Srinivasan; ESWARAIAH, Sajja; RAGHURAM, Suraparaju; SEETHA RAMA SARMA, Peri
Patent: WO2012/98560 A2, 2012 ;
WO 2012/098560 A2
反应条件
1.1: thionyl chloride / 10 °C / Reflux 2.1: lithium aluminium tetrahydride / tetrahydrofuran / 14 h / 25 - 30 °C 3.1: hydrogen / 5 Pd(II)/C(eggshell) / methanol / 50 - 55 °C 4.1: dichloromethane / 1.5 h / 0 - 5 °C 4.2: 1 h / 0 - 5 °C View Scheme
反应条件
1: With thionyl chloride T=10°C; Reflux; 2: With sodium hydrogencarbonate in dichloromethane; water
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; THIRUMALAI RAJAN, Srinivasan; ESWARAIAH, Sajja; RAGHURAM, Suraparaju; SEETHA RAMA SARMA, Peri
Patent: WO2012/98560 A2, 2012 ;
Location in patent: Page/Page column 56-57 ;
WO 2012/098560 A2