4-氯吡啶-2-甲酸甲酯合成路线 (共 44 条)
反应条件
1: pyridine-2-carboxylic acid With thionyl chloride; N,N-dimethyl-formamide T=20 - 72°C; 16.6667 h; 2: methanol T=20 - 55°C; 0.75 h; 3: With water; sodium hydrogencarbonate in methanol T=45°C; pH=8 - 9;
参考文献
Cai, Xiong; Qian, Changgeng; Gould, Stephen; Zhai, Haixiao
Patent: US2008/234332 A1, 2008 ;
Location in patent: Page/Page column 22; 25 ;
US 20080234332 A1
反应条件
1: 4-chloro-2-pyridinecarboxylic acid With oxalyl dichloride; N,N-dimethyl-formamide in dichloromethane T=0 - 20°C; 2: methanol T=20°C; 0.5 h;
参考文献
F. HOFFMANN-LA ROCHE LTD; EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL); SAVIRA PHARMACEUTICALS GMBH; CLASSEN-HOUBEN, Dirk; WOLKERSTORFER, Andrea; SZOLAR, Oliver; SMITH, Mark; SO, Sung-Sau; CUSACK, Stephen; LANGER, Thierry; GIETHLEN, Bruno; MORICE, Christophe; MICHAUT-SIMON, Céline; ZUBIETA, Chloe
Patent: US2013/102600 A1, 2013 ;
Location in patent: Paragraph 0160; 0161 ;
反应条件
1: pyridine-2-carboxylic acid With thionyl chloride T=20 - 100°C; 157.333 h; 2: methanol T=0 - 20°C; 18.5 h; 3: With sodium hydroxide in tetrahydrofuran; water; ethyl acetate
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1889836 A1, 2008 ;
Location in patent: Page/Page column 45 ;
反应条件
sodium bromide in methanol; thionyl chloride; sodium hydrogencarbonate
参考文献
Lewis, Jason G.; Anandan, Sampath K.; O'Dowd, Hardwin; Gordeev, Mikhail F.
Patent: US2005/215488 A1, 2005 ;
反应条件
1: With methanol in tetrahydrofuran T=0 - 20°C; 2: With acetic acid in tetrahydrofuran; methanol; water
参考文献
THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH; LUDWIG INSTITUTE FOR CANCER RESEARCH LIMITED; LESSENE, Guillaume Laurent; BAELL, Jonathan Bayldon; BURGESS, Antony Wilks; MARUTA, Hiroshi
Patent: WO2012/3544 A1, 2012 ;
Location in patent: Page/Page column 78 ;
WO 2012/003544 A1
参考文献
VICURON PHARMACEUTICALS, INC.
Patent: WO2004/16632 A2, 2004 ;
Location in patent: Page 57-58 ;
反应条件
in toluene T=0°C; 1 h;
参考文献
MERCK PATENT GmbH
Patent: WO2005/82853 A1, 2005 ;
Location in patent: Page/Page column 200-201 ;
WO 2005/082853 A1
反应条件
thionyl chloride in methanol; water; toluene
反应条件
1,8-diazabicyclo[5.4.0]undec-7-ene in acetonitrile 48 h;
参考文献
US2004/186114 A1, ;
Page/Page column 61; 62; 64 ;
反应条件
1: mCPBA / CH2Cl2 / 48 h / Ambient temperature 2: POCl3 / 17 h / 80 °C View Scheme
参考文献
Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 39, # 6 p. 455 - 460