(1R)-3-(4-吗啉)-3-氧代-1-((苯基磺酰基)甲基)丙基氨基甲酸苄酯合成路线 （共 7 条）
反应条件
1: With hydrogen bromide; acetic acid T=18 - 25°C; 50 h; 2: With sodium carbonate in water pH=~ 8 - 9;
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
Location in patent: Page/Page column 57 ;
反应条件
tributylphosphine in toluene
T=80°C; 24 h;
参考文献
Elmore, Steven W.; Bruncko, Milan; Park, Cheol-Min
Patent: US2005/272744 A1, 2005 ;
Location in patent: Page/Page column 20 ;
US 20050272744 A1
反应条件
1: thiophenol With sodium hydride in tetrahydrofuran
T=0 - 10°C; 1 h;
2: C17H24N2O7S in tetrahydrofuran
T=0 - 20°C; 1.5 h;
参考文献
GENENTECH, INC.; WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH
Patent: WO2008/61208 A2, 2008 ;
Location in patent: Page/Page column 31; 33 ;
WO 2008/061208 A2
反应条件
1.1: sodium tetrahydroborate / tetrahydrofuran / 6 h / 0 - 25 °C
1.2: 0 °C / pH 4
2.1: toluene-4-sulfonic acid / toluene / 3 h / Dean-Stark conditions; Reflux
3.1: tetrahydrofuran / 18 - 25 °C
4.1: tributylphosphine / toluene / 80 °C / Inert atmosphere
View Scheme
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
反应条件
1: tetrahydrofuran / 18 - 25 °C
2: tributylphosphine / toluene / 80 °C / Inert atmosphere
View Scheme
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
反应条件
1: toluene-4-sulfonic acid / toluene / 3 h / Dean-Stark conditions; Reflux
2: tetrahydrofuran / 18 - 25 °C
3: tributylphosphine / toluene / 80 °C / Inert atmosphere
View Scheme
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
反应条件
1.1: acetic anhydride / 18 - 25 °C
2.1: sodium tetrahydroborate / tetrahydrofuran / 6 h / 0 - 25 °C
2.2: 0 °C / pH 4
3.1: toluene-4-sulfonic acid / toluene / 3 h / Dean-Stark conditions; Reflux
4.1: tetrahydrofuran / 18 - 25 °C
5.1: tributylphosphine / toluene / 80 °C / Inert atmosphere
View Scheme
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
