2-氨基-6,7-二氢噻唑并[5,4-c]吡啶-5(4H)-甲酸叔丁酯合成路线 （共 14 条）
反应条件
toluene-4-sulfonic acid; sulfur in methanol T=0 - 20°C; 5 h;
参考文献
EP1405852 A1, ;
Page 65 ;
EP 1405852 A1
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With pyrrolidine; toluene-4-sulfonic acid in cyclohexane 5 h; Heating / reflux; 2: acetamide With sulfur in methanol T=4°C; 2 h; Cooling with ice;
参考文献
WO2008/86047 A1, ;
Page/Page column 127-128 ;
WO 2008/086047 A1
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With pyrrolidine; toluene-4-sulfonic acid in cyclohexane 2 h; Heating; 2: Carbamonitrile With sulfur in methanol T=0°C; 5 h;
参考文献
Haginoya, Noriyasu; Komoriya, Satoshi; Osanai, Ken; Yoshino, Toshiharu; Nagata, Tsutomu; Nagamochi, Masatoshi; Muto, Ryo; Yamaguchi, Mitsuhiro; Nagahara, Takayasu; Kanno, Hideyuki
Heterocycles, 2004 , vol. 63, # 7 p. 1555 - 1561
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With pyrrolidine; toluene-4-sulfonic acid in cyclohexane 2 h; Heating / reflux; 2: Carbamonitrile With sulfur in methanol T=0 - 20°C; 5 h;
参考文献
EP1577301 A1, ;
Page/Page column 72 ;
反应条件
1: in acetone T=20°C; 2: With triethylamine in acetone 0.333333 h;
参考文献
WO2006/108709 A1, ;
Page/Page column 69 ;
WO 2006/108709 A1
反应条件
potassium carbonate in 1,4-dioxane; water T=0 - 20°C; 3 h;
参考文献
GRAUERT, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KUELZER, Raimund; RUDOLF, Klaus; WELLENZOHN, Bernd
Patent: US2013/150341 A1, 2013 ;
Location in patent: Paragraph 0179; 0180; 0181 ;
反应条件
potassium carbonate in 1,4-dioxane; water T=20°C; 3 h; Enzymatic reaction;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; GRAUERT, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KUELZER, Raimund; RUDOLF, Klaus; WELLENZOHN, Bernd
Patent: WO2013/83741 A1, 2013 ;
Location in patent: Page/Page column 61 ;
反应条件
1: thiourea; tert-butyl 3-bromo-4-oxo-piperidine-1-carboxylate With potassium carbonate in acetone T=20°C; 12 h; 2: di-tert-butyl dicarbonate in acetone 4 h;
参考文献
WO2007/95124 A2, ;
Page/Page column 63-64 ;
反应条件
sulfur; Carbamonitrile in pyridine 1.66667 h; Heating / reflux;
参考文献
WO2004/43968 A1, ;
Page 22 ;
WO 2004/043968 A1
反应条件
1: hydrogen bromide; acetic acid; bromine / 0.75 h / 20 °C 2: ethanol / 20 h / |Reflux 3: potassium carbonate / 1,4-dioxane; water / 3 h / 20 °C / |Enzymatic reaction View Scheme
