(2R)-2-(环戊氨基)-丁酸甲酯合成路线 (共 5 条)
反应条件
1.1: potassium carbonate / acetone / 0 - 20 °C / Inert atmosphere 2.1: iron / acetic acid / 2.5 h / 70 - 100 °C / Inert atmosphere 3.1: sodium hydride / isobutyramide; mineral oil / -10 - 20 °C / Inert atmosphere 4.1: hydrogenchloride / ethanol; water / 48 h / Inert atmosphere; Reflux 5.1: O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; diisopropylamine / N,N-dimethyl-formamide / 0.5 h / 20 °C / Inert atmosphere 5.2: 3 h / 20 °C / Inert atmosphere View Scheme
参考文献
Budin, Ghyslain; Yang, Katherine S.; Reiner, Thomas; Weissleder, Ralph
Angewandte Chemie - International Edition, 2011 , vol. 50, # 40 p. 9378 - 9381
反应条件
sodium acetate; sodium tris(acetoxy)borohydride in dichloromethane
T=0 - 20°C; Inert atmosphere;
参考文献
Budin, Ghyslain; Yang, Katherine S.; Reiner, Thomas; Weissleder, Ralph
Angewandte Chemie - International Edition, 2011 , vol. 50, # 40 p. 9378 - 9381
反应条件
1: (R)-methyl 2-(cyclopentylamino)butanoate With sodium hydrogencarbonate in cyclohexane
T=20 - 30°C; 0.5 h;
2: 2,4-Dichloro-5-nitro-pyrimidine in cyclohexane
T=60°C; 12 h; Inert atmosphere;
参考文献
SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.; JIANGSU HENGRUI MEDICINE CO., LTD.
Patent: US2012/184543 A1, 2012 ;
Location in patent: Page/Page column 24 ;
反应条件
1: potassium carbonate / acetone / 16 h / 0 °C
2: hydrogen; acetic acid / Raney Ni / 50 °C
View Scheme
参考文献
Jiangsu Hengrui Medicine Co., Ltd.; Shanghai Hengrui Pharmaceutical Co. Ltd.
Patent: EP2481739 A1, 2012 ;
反应条件
1: potassium carbonate / acetone / 0 - 20 °C / Inert atmosphere
2: iron / acetic acid / 2.5 h / 70 - 100 °C / Inert atmosphere
3: sodium hydride / isobutyramide; mineral oil / -10 - 20 °C / Inert atmosphere
4: hydrogenchloride / ethanol; water / 48 h / Inert atmosphere; Reflux
View Scheme
参考文献
Budin, Ghyslain; Yang, Katherine S.; Reiner, Thomas; Weissleder, Ralph
Angewandte Chemie - International Edition, 2011 , vol. 50, # 40 p. 9378 - 9381