1-BOC-哌啶-3-羧酸合成路线 （共 37 条）
反应条件
1: N-tert-butoxycarbonyl-3-piperidinecarboxylic acid With pyridine; thionyl chloride in dichloromethane
T=25°C; 0.333333 h;
2: 2,2-Dimethyl-[1,3]dioxane-4,6-dione With 4-(N,N-dimethlyamino)pyridine in dichloromethane
1 h;
3: in methanol
4 h; Heating / reflux;
参考文献
SCHERING CORPORATION
Patent: WO2009/70567 A1, 2009 ;
Location in patent: Page/Page column 60 ;
WO 2009/070567 A1
反应条件
1: N-tert-butoxycarbonyl-3-piperidinecarboxylic acid With pyridine; thionyl chloride in dichloromethane
T=25°C; 0.333333 h;
2: 2,2-Dimethyl-[1,3]dioxane-4,6-dione With 4-(N,N-dimethlyamino)pyridine in dichloromethane
1 h;
3: methanol 4 h; Heating / reflux;
参考文献
Schering Corporation
Patent: US2007/83044 A1, 2007 ;
Location in patent: Page/Page column 32 ;
US 20070083044 A1
反应条件
1: 1.) Et3N, ClCO2C2H5; 2.) NH3 / 1.) chloroform, 0 deg C, 8 min; 2.) chloroform, RT, 2-4 h
2: POCl3 / pyridine
3: 50 percent / NaN3, NH4Cl / dimethylformamide / 100 °C
View Scheme
参考文献
Schlewer; Wermuth; Chambon
European Journal of Medicinal Chemistry, 1984 , vol. 19, # 2 p. 181 - 186
反应条件
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in dichloromethane
T=20°C;
参考文献
Zhang, Li; Qiu, Beiying; Xiong, Bing; Li, Xin; Li, Jingya; Wang, Xin; Li, Jia; Shen, Jingkang
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 8 p. 2118 - 2122
反应条件
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in dichloromethane
T=20°C;
参考文献
Zhang, Li; Qiu, Beiying; Xiong, Bing; Li, Xin; Li, Jingya; Wang, Xin; Li, Jia; Shen, Jingkang
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 8 p. 2118 - 2122
反应条件
1.1: potassium carbonate / N,N-dimethyl-formamide / 3 h / 20 °C
2.1: lithium hexamethyldisilazane / tetrahydrofuran / 0.7 h / -72 - 0 °C
2.2: 3 h / -67 - 2.5 °C
View Scheme
参考文献
JAPAN TOBACCO INC.
Patent: US2011/136778 A1, 2011 ;
US 20110136778 A1
反应条件
1: benzotriazole-1-yl-oxy-tris(dimethylamino)phosphonium*PF6(1-; N-hydroxybenzotriazole (HOBt); DIEA
2: 30 percent TFA / CH2Cl2
View Scheme
参考文献
Baek, Bong-Hyeon; Lee, Myung-Ryul; Kim, Kwang-Yon; Cho, Ung-In; Boo, Doo Wan; Shin, Injae
Tetrahedron Letters, 2003 , vol. 44, # 17 p. 3447 - 3450
