反应条件
1.1: hydrogenchloride; water / tert-butyl methyl ether / 1 h / 22 - 25 °C / pH 0.5 - 0.6 / Industry scale
1.2: 0.25 h / 22 - 30 °C / pH >= 12 / Industry scale
2.1: N-ethyl-N,N-diisopropylamine / tert-butyl methyl ether / 1 h / 2 °C / Industry scale
3.1: tetramethyl guanidine / isopropyl alcohol / 1.5 h / 70 °C / Industry scale
3.2: 22 °C / pH <= 1.5 / Industry scale
4.1: benzotriazol-1-ol; 4-methyl-morpholine; N'-(3-dimethylaminopropyl)-N-ethylcarbodiimide / acetonitrile; water / 5 h / 5 - 40 °C / Industry scale
5.1: sodium hydroxide; water / 2-methyl tetrahydrofuran / 7 h / 20 - 60 °C / Industry scale
5.2: 0.17 h / 20 - 30 °C / pH 1.5 - 3 / Industry scale
View Scheme
参考文献
SCHERING CORPORATION; TRAVERSE, John; LEONG, William, W.; MILLER, Steven, P.; ALBANEZE-WALKER, Jennifer; HUNTER, Thomas, J.; WANG, Lijun; LIAO, Hongbiao; ARASAPPAN, Ashok; TRZASKA, Scott, T.; SMITH, Randi, M.; LEKHAL, Azzeddine; BOGEN, Stephane, L.; KONG, Jianshe; BENNETT, Frank; NJOROGE, F., George; POIRIER, Marc; KUO, Shen-Chun; CHEN, Yonggang; MATTHEWS, Kenneth S.; DEMONCHAUX, Patrice; FERREIRA, Amadeo
Patent: WO2011/14494 A1, 2011 ;
