2-(1-(4-乙酰氨基苯基)-1-氧代丙烷-2-基)丙二酸二乙酯合成路线 （共 8 条）
反应条件
1: 1.) HCl/EtOH, 2.) 6N aq. HCl / 2 h / Heating; 1.) reflux, 2 h, 2.) reflux, 2 h 2: 87 percent / hydrazine hydrate / H2O / 1.5 h / Heating View Scheme
参考文献
Burpitt; Crawford; Davies; Mistry; Mitchell; Pancholi; Coates
Journal of Heterocyclic Chemistry, 1988 , vol. 25, # 6 p. 1689 - 1695
反应条件
1.1: sodium hydroxide / water / 4 h 1.2: 3 h / 100 °C / pH 1 2.1: L-(+)-tartaric acid / isopropyl alcohol / 0.5 h / Heating; Resolution of racemate 2.2: pH 7 - 8 / Resolution of racemate 2.3: 0.5 h / Reflux; Resolution of racemate View Scheme
参考文献
Wang, Lisheng; Zhou, Hongxiang; Yang, Bin; Chen, Zhigang; Yang, Hua
Medicinal Chemistry Research, 2011 , vol. 20, # 3 p. 287 - 292
反应条件
hydrogenchloride; ethanol 2 h; Heating1.) reflux, 2 h, 2.) reflux, 2 h; Yield given;
参考文献
Burpitt; Crawford; Davies; Mistry; Mitchell; Pancholi; Coates
Journal of Heterocyclic Chemistry, 1988 , vol. 25, # 6 p. 1689 - 1695
反应条件
1: diethyl malonate With sodium hydride in N,N-dimethyl-formamide
T=50°C; 1.5 h;
2: N-[4-(2-chloro-1-oxopropyl)phenyl]acetamide in N,N-dimethyl-formamide
T=80°C; 3 h;
3: With water in N,N-dimethyl-formamide
参考文献
Boehringer Ingelheim Pharma GmbH and Co. KG
Patent: US7230001 B1, 2007 ;
Location in patent: Page/Page column 87 ;
US 7230001 B1
反应条件
1: diethyl malonate With sodium hydride in tetrahydrofuran
cooling;
2: N-(4-(2-bromopropionyl)phenyl)acetamide in tetrahydrofuran
T=20°C; 5 h; Further stages.;
参考文献
Wang, Teng; Dong, Ying; Wang, Li-Chen; Chen, Zhen
Arzneimittel-Forschung/Drug Research, 2007 , vol. 57, # 10 p. 641 - 646
反应条件
1: 61 percent / AlCl3 / CH2Cl2 / Ambient temperature; overnight
2: 1) NaH / 1) DMF, room temperature, overnight, 2) DMF, 110 deg C, 3 h
View Scheme
参考文献
Burpitt; Crawford; Davies; Mistry; Mitchell; Pancholi; Coates
Journal of Heterocyclic Chemistry, 1988 , vol. 25, # 6 p. 1689 - 1695
反应条件
1.1: bromine / chloroform
1.2: 24 h / 20 °C / pH 8
2.1: sodium ethanolate / ethanol / Cooling with ice
2.2: 8.17 h / 35 - 75 °C
View Scheme
参考文献
Wang, Lisheng; Zhou, Hongxiang; Yang, Bin; Chen, Zhigang; Yang, Hua
Medicinal Chemistry Research, 2011 , vol. 20, # 3 p. 287 - 292
反应条件
1: 1.) HCl/EtOH, 2.) 6N aq. HCl / 2 h / Heating; 1.) reflux, 2 h, 2.) reflux, 2 h
2: 87 percent / hydrazine hydrate / H2O / 1.5 h / Heating
View Scheme
参考文献
Burpitt; Crawford; Davies; Mistry; Mitchell; Pancholi; Coates
Journal of Heterocyclic Chemistry, 1988 , vol. 25, # 6 p. 1689 - 1695
