2-溴-2-(2-氟苯基)-1-环丙基乙酮合成路线 （共 21 条）
反应条件
1: 5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H)-one hydrochloride With potassium carbonate in acetonitrile T=25 - 30°C; 0.5 h; 2: α-cyclopropylcarbonyl-2-fluorobenzyl bromide in acetonitrile T=25 - 30°C; 6 h; 3: acetic anhydride With triethylamine in acetonitrile T=0 - 30°C; 6.5 h;
参考文献
WO2011/42918 A2, ;
Page/Page column 48-49 ;
反应条件
1: α-cyclopropylcarbonyl-2-fluorobenzyl bromide; 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one p-toluenesulfonate With N-ethyl-N,N-diisopropylamine in acetonitrile T=30°C; 0.5 h; 2: acetic anhydride With N-ethyl-N,N-diisopropylamine; 4-(N,N-dimethlyamino)pyridine in acetonitrile Product distribution / selectivity;
参考文献
WO2011/57592 A1, ;
Page/Page column 12 ;
反应条件
1: With potassium carbonate in acetonitrile T=25 - 30°C; 6.5 h; 2: With acetic anhydride; triethylamine in acetonitrile T=0 - 30°C; 6.5 h; 3: With water in acetonitrile
参考文献
US2012/202066 A1, ;
Page/Page column 22-23 ;
反应条件
triethylamine in dichloromethane T=-15 - 20°C; Product distribution / selectivity;
参考文献
WO2011/29456 A1, ;
Page/Page column 17 ;
反应条件
1.1: potassium carbonate / acetonitrile / 5 h / 25 - 35 °C 2.1: lithium diisopropyl amide / tetrahydrofuran / 1 h / -78 °C 2.2: 1 h / -78 °C 2.3: 1 h / -60 - 0 °C 3.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 3.33 h / 10 - 30 °C View Scheme
反应条件
1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 20 °C / Cooling with ice 2: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 15 - 25 °C View Scheme
反应条件
ammonium hydrogen carbonate in dichloromethane T=5 - 20°C;
参考文献
MAYUKA LABS PVT. LTD.; KRISHNAMURTHY, Chandra, Sekhar, Nakka; SINGH, Jagat; KHAN, Mohd, Yunus
Patent: WO2012/1486 A1, 2012 ;
Location in patent: Page/Page column 22 ;
反应条件
sodium carbonate in N,N-dimethyl-formamide T=0 - 5°C; 3 h; Product distribution / selectivity;
参考文献
MSN LABORATORIES LIMITED
Patent: WO2009/66326 A2, 2009 ;
Location in patent: Page/Page column 20 ;
反应条件
triethylamine in tetrahydrofuran T=0 - 5°C; 3 h; Product distribution / selectivity;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.; ANUMULA, Raghupathi Reddy; GILLA, Goverdhan; AALLA, Sampath; METIL, Dattatray, Shamrao; KURELLA, Srinivas; CHARAGONDLA, Kavitha
Patent: WO2012/18791 A2, 2012 ;
Location in patent: Page/Page column 28-29 ;
反应条件
sodium carbonate in tetrahydrofuran T=0 - 5°C; 5 h; Product distribution / selectivity;
参考文献
MSN LABORATORIES LIMITED
Patent: WO2009/66326 A2, 2009 ;
Location in patent: Page/Page column 16 ;
