1-苄基哌嗪-2-羧酸乙酯合成路线 (共 7 条)
反应条件
1-chloroethyl chlorocarbonate in 1,2-dichloro-ethane T=0°C; 1.16667 h; Heating / reflux;
参考文献
ASTEX TECHNOLOGY LIMITED; CANCER RESEARCH TECHNOLOGY LIMITED; THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
Patent: WO2005/11697 A2, 2005 ;
Location in patent: Page/Page column 52; 82-83 ;
WO 2005/011697 A2
反应条件
hydrogenchloride in acetone 3 h; Ambient temperature;
参考文献
Rondu, Frederic; Bihan, Gaelic Le; Wang, Xuan; Lamouri, Aazdine; Touboul, Estera; Dive, Georges; Bellahsene, Tounes; Pfeiffer, Bruno; Renard, Pierre; Guardiola-Lemaitre, Beatrice; Manechez, Dominique; Penicaud, Luc; Ktorza, Alain; Godfroid, Jean-Jacques
Journal of Medicinal Chemistry, 1997 , vol. 40, # 23 p. 3793 - 3803
反应条件
1: K2CO3, KI / acetone / 15 h / Ambient temperature 2: conc. HCl / acetone / 3 h / Ambient temperature View Scheme
参考文献
Rondu, Frederic; Bihan, Gaelic Le; Wang, Xuan; Lamouri, Aazdine; Touboul, Estera; Dive, Georges; Bellahsene, Tounes; Pfeiffer, Bruno; Renard, Pierre; Guardiola-Lemaitre, Beatrice; Manechez, Dominique; Penicaud, Luc; Ktorza, Alain; Godfroid, Jean-Jacques
Journal of Medicinal Chemistry, 1997 , vol. 40, # 23 p. 3793 - 3803
反应条件
1: triethylamine / toluene / 12.5 h / 25 - 80 °C 2: 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.75 h / 0 - 90 °C View Scheme
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; REN, Qingyun; LIU, Xinchang; SIEGFRIED, Goldmann
Patent: WO2014/29193 A1, 2014 ;
反应条件
1: With lithium aluminium tetrahydride in tetrahydrofuran
T=0 - 20°C; 2 h; Inert atmosphere;
2: With water; sodium hydroxide in tetrahydrofuran
T=0°C;
3: With potassium carbonate in tetrahydrofuran; water
T=20°C; 0.333333 h;
参考文献
SK CHEMICALS CO. LTD.; Kim, Seon Mi; Lee, Min Hee; Kim, Jae Sun; Jung, Hoe Chul; Lee, So Young; Lee, Soo Min; Kim, Eun Jeong; Park, Eui Sun; Park, Sung Hoon; Lee, Bong Yong; Um, Key An
Patent: US2013/137661 A1, 2013 ;
Location in patent: Paragraph 0191 ;
反应条件
formic acid in methanol; water
20 h; Heating;
参考文献
Rondu, Frederic; Bihan, Gaelic Le; Wang, Xuan; Lamouri, Aazdine; Touboul, Estera; Dive, Georges; Bellahsene, Tounes; Pfeiffer, Bruno; Renard, Pierre; Guardiola-Lemaitre, Beatrice; Manechez, Dominique; Penicaud, Luc; Ktorza, Alain; Godfroid, Jean-Jacques
Journal of Medicinal Chemistry, 1997 , vol. 40, # 23 p. 3793 - 3803
反应条件
1: 94 percent / Et3N / CH2Cl2 / 1.) -75 deg C, 1 h, 2.) -> r.t.
2: 69 percent / H2 / 10percent Pd-C / acetic acid / 1 h / 2068.6 Torr / Ambient temperature
3: 82 percent / NaHCO3 / CH2Cl2 / 3 h / 0 °C
4: 52 percent / ethanol / 1 h / 0 °C
5: 58 percent / LiAlH4 / tetrahydrofuran / 18 h / Heating
View Scheme
参考文献
Gubert; Braojos; Sacristan; Ortiz
Synthesis, 1991 , # 4 p. 318 - 320