(1R,2S)-REL-1-[[(1,1-二甲基乙氧基)羰基]氨基]-2-乙烯基-环丙羧酸乙酯合成路线 （共 8 条）
反应条件
sodium hydroxide; Alcalase in water; dimethyl sulfoxide T=39 - 40°C; pH=8; 67.1667 h; Sodium phosphate buffer; Product distribution / selectivity;
参考文献
US2008/14173 A1, ;
Page/Page column 22-23 ;
US 20080014173 A1
反应条件
Savinase in dimethyl sulfoxide T=40°C; pH=8.5; 18 h; Heps. Na buffer; Product distribution / selectivity;
参考文献
US2008/14173 A1, ;
Page/Page column 22-23 ;
US 20080014173 A1
反应条件
T=20°C; Heating / reflux;
参考文献
US2008/107624 A1, ;
Page/Page column 20 ;
反应条件
1: various solvent(s); toluene / 17.5 h / 20 °C 2: Alcalase 2.4L; NaOH / acetone; H2O / 216 h / 40 °C / pH 7.5 - 8.5 View Scheme
参考文献
Journal of Organic Chemistry, , vol. 70, # 15 p. 5869 - 5879
反应条件
sulfuric acid in water pH=2;
参考文献
REF PHARMA, LLC.; COATS, Steven, J.
Patent: WO2013/106689 A1, 2013 ;
Location in patent: Page/Page column 24 ;
反应条件
1: With sulfuric acid; water in ethyl acetate
T=20 - 48°C; 1 h;
2: With triethylamine in ethyl acetate
T=18 - 30°C;
参考文献
Roche Palo Alto LLC
Patent: US2009/163706 A1, 2009 ;
Location in patent: Page/Page column 11 ;
US 20090163706 A1
反应条件
1: ethyl (1R,2S)-N-(tert-butyloxycarbonyl)-1-amino-2-vinylcyclopropanecarboxylate With 1,1'-carbonyldiimidazole in tetrahydrofuran
0.833333 h; Heating / reflux;
2: cyclopropanesulfonic acid amide With 1,8-diazabicyclo[5.4.0]undec-7-ene in tetrahydrofuran
T=20°C; 20 h;
参考文献
BRISTOL-MYERS SQUIBB COMPANY
Patent: WO2008/64057 A1, 2008 ;
Location in patent: Page/Page column 63 ;
反应条件
1.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 20 °C
2.1: 4-(N,N-dimethlyamino)pyridine; HATU / dichloromethane / 1 h / 20 °C
2.2: 20 °C
View Scheme
参考文献
REF PHARMA, LLC.; COATS, Steven, J.
Patent: WO2013/106689 A1, 2013 ;
