3-(3,4-二氯苯基)丙酸合成路线 （共 16 条）
反应条件
1.1: borane-THF / tetrahydrofuran / 12 h / 0 °C 2.1: methanesulfonyl chloride / pyridine / 3 h / 20 °C 2.2: 72 h / 0 - 20 °C 3.1: water; sodium hydroxide / ethanol / 3 h / |Reflux View Scheme
参考文献
BRISTOL-MYERS SQUIBB COMPANY; ABELL, Lynn; ADAM, Leonard; CAVALLARO, Cullen L.; FINLAY, Heather; FRIENDS, Todd J.; HANGELAND, Jon J.; JIANG, Ji; LAWRENCE, R. Michael; LLOYD, John; PI, Zulan; TORA, George O.; QIAO, Jennifer X.; HU, Carol Hui; WANG, Tammy C.
Patent: WO2013/48982 A1, 2013 ;
反应条件
thionyl chloride; aluminium trichloride in dichloromethane
参考文献
Roussel Uclaf
Patent: US5348971 A1, 1994 ;
反应条件
trifluorormethanesulfonic acid T=100°C; 24 h;
参考文献
Astellas Pharma Inc.
Patent: EP1795524 A1, 2007 ;
Location in patent: Page/Page column 22-23 ;
EP 1795524 A1
反应条件
1: thionyl chloride / toluene / 3 h / 55 - 60 °C 2: 1.) aq. sodium azide / 1.) acetone, 0 deg C, 0.5 h, 2.) toluene, 80 deg C, 0.5 h View Scheme
参考文献
Anderson, Wayne K.; Heider, Arvela R.; Raju, Natarajan; Yucht, Jeffery A.
Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2097 - 2102
反应条件
1: triethylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C
2: diethyl ether / 19 h / 0 - 20 °C
View Scheme
参考文献
BRISTOL-MYERS SQUIBB COMPANY; ABELL, Lynn; ADAM, Leonard; CAVALLARO, Cullen L.; FINLAY, Heather; FRIENDS, Todd J.; HANGELAND, Jon J.; JIANG, Ji; LAWRENCE, R. Michael; QIAO, Jennifer X.; HU, Carol Hui; WANG, Tammy C.
Patent: WO2013/49096 A1, 2013 ;
反应条件
1.1: oxalyl dichloride; N,N-dimethyl-formamide / dichloromethane / 3.5 h / 0 - 20 °C
1.2: 2 h / 0 - 20 °C
2.1: lithium aluminium tetrahydride / tetrahydrofuran / 7.17 h / 0 - 20 °C / |Inert atmosphere
3.1: triethylamine / tetrahydrofuran / 16 h / 20 °C
4.1: hydrogenchloride / 1,4-dioxane / 2 h / 20 °C
View Scheme
参考文献
BRISTOL-MYERS SQUIBB COMPANY; HU, Carol Hui; QIAO, Jennifer X.; WANG, Tammy C.
Patent: WO2013/151923 A1, 2013 ;
