5-(2-氨基丙基)-1-[3-(苯甲酰氧基)丙基]-2,3-二氢-1H-吲哚-7-甲腈合成路线 (共 6 条)
反应条件
pyridoxal 5'-phosphate; sodium 2-oxopropanoate in aq. phosphate buffer; dimethyl sulfoxide T=30°C; pH=7; 24 h; Resolution of racemateSchlenk techniqueInert atmosphereEnzymatic reaction; Reagent/catalyst;
参考文献
Simon, Robert C.; Sattler, Johann H.; Farnberger, Judith E.; Fuchs, Christine S.; Richter, Nina; Zepeck, Ferdinand; Kroutil, Wolfgang
Tetrahedron Asymmetry, 2014 , vol. 25, # 3 p. 284 - 288
反应条件
1: water; acetone / 3.25 h / 20 °C / Reflux 2: sodium carbonate / water / pH 8 - 9 View Scheme
参考文献
Simon, Robert C.; Sattler, Johann H.; Farnberger, Judith E.; Fuchs, Christine S.; Richter, Nina; Zepeck, Ferdinand; Kroutil, Wolfgang
Tetrahedron Asymmetry, 2014 , vol. 25, # 3 p. 284 - 288
反应条件
1: water; acetone / 3.25 h / 20 °C / Reflux 2: sodium carbonate / water / pH 8 - 9 3: sodium carbonate / ethanol; tert-butyl alcohol / 42 h / 50 - 90 °C 4: sodium hydroxide; water / methanol / 1.25 h / 20 °C / cooling with ice View Scheme
参考文献
RATIOPHARM GMBH; GIDWANI, Ramesh Matioram; KOLHATKAR, Mayur Vilas
Patent: WO2011/124704 A1, 2011 ;
反应条件
1: water; acetone / 3.25 h / 20 °C / Reflux 2: sodium carbonate / water / pH 8 - 9 3: sodium carbonate / ethanol; tert-butyl alcohol / 42 h / 50 - 90 °C 4: sodium hydroxide; water / methanol / 1.25 h / 20 °C / cooling with ice 5: sodium hydroxide; dihydrogen peroxide / water; dimethyl sulfoxide / 2.25 h / 20 - 25 °C View Scheme
参考文献
RATIOPHARM GMBH; GIDWANI, Ramesh Matioram; KOLHATKAR, Mayur Vilas
Patent: WO2011/124704 A1, 2011 ;
反应条件
in water; acetone T=25 - 65°C; Resolution of racemate;
参考文献
SANDOZ AG; KUMAR LUTHRA, Parven; BHUTA, Sachin; ABHINAY, Chandrakant Pise; DATTATRAYA, N., Chavan; SHASHIKANT, D., Metkar
Patent: WO2013/56842 A1, 2013 ;
Location in patent: Page/Page column 19; 20 ;
反应条件
in tetrahydrofuran; water T=20 - 65°C; Product distribution / selectivity;
参考文献
PANACEA BIOTEC LTD; JAIN, Rajesh; RAO, Jagadeeshwar R; RAO, Siripragada Mahender
Patent: WO2012/131710 A2, 2012 ;
Location in patent: Page/Page column 32-33 ;