乙基3-(3-氯苯基)-5-甲基-1,2-恶唑-4-羧酸酯合成路线 （共 7 条）
反应条件
1: ethyl acetoacetate With sodium in methanol
T=20°C; 0.25 h;
2: N-hydroxy-3-chloro-benzenecarboximidoyl chloride in methanol
T=20°C; 4.33333 h;
参考文献
F. HOFFMANN-LA ROCHE AG; DOTT, Pascal; HANLON, Steven Paul; HILDBRAND, Stefan; IDING, Hans; THOMAS, Andrew; WALDMEIER, Pius
Patent: WO2013/57123 A1, 2013 ;
Location in patent: Page/Page column 32 ;
反应条件
triethylamine in ethanol
T=0 - 20°C;
参考文献
Gerritz, Samuel; Shi, Shuhao; Zhu, Shirong
Patent: US2006/287287 A1, 2006 ;
Location in patent: Page/Page column 22 ;
US 20060287287 A1
反应条件
triethylamine in ethanol
T=20°C;
参考文献
Zamponi, Gerald W.; Stotz, Stephanie C.; Staples, Richard J.; Andro, Tina M.; Nelson, Jared K.; Hulubei, Victoria; Blumenfeld, Alex; Natale, Nicholas R.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 1 p. 87 - 96
反应条件
1: N-chloro-succinimide / N,N-dimethyl-formamide / 20 °C
2: triethylamine / ethanol; N,N-dimethyl-formamide / 16 h / 20 °C
View Scheme
参考文献
Zhu, Shirong; Shi, Shuhao; Gerritz, Samuel W.
Tetrahedron Letters, 2011 , vol. 52, # 31 p. 4001 - 4004
反应条件
1: hydroxylamine hydrochloride; triethylamine / N,N-dimethyl-formamide / 1 h / 20 °C
2: N-chloro-succinimide / N,N-dimethyl-formamide / 20 °C
3: triethylamine / ethanol; N,N-dimethyl-formamide / 16 h / 20 °C
View Scheme
参考文献
Zhu, Shirong; Shi, Shuhao; Gerritz, Samuel W.
Tetrahedron Letters, 2011 , vol. 52, # 31 p. 4001 - 4004
反应条件
sodium hydroxide in methanol
参考文献
Xin, Zhili; Zhao, Hongyu; Serby, Michael D.; Liu, Bo; Schaefer, Verlyn G.; Falls, Douglas H.; Kaszubska, Wiweka; Colins, Christine A.; Sham, Hing L.; Liu, Gang
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 4 p. 1201 - 1204
反应条件
lithium aluminium tetrahydride in tetrahydrofuran
T=0°C;
参考文献
Zamponi, Gerald W.; Stotz, Stephanie C.; Staples, Richard J.; Andro, Tina M.; Nelson, Jared K.; Hulubei, Victoria; Blumenfeld, Alex; Natale, Nicholas R.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 1 p. 87 - 96
