| Novel Method for Selective Debenzylation Under Maintenance of Fluoro Atom Substituted on β-Amino Acids |
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| 基金项目： | Supported by the National Key New Drug Creation Program of China(No.2009ZX09103-001); the Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research Foundation, China(No.BM2008201) |
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| 摘 要： |
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| 关 键 词： | β-Amino acid Debenzylation Defluorination Catalytic hydrogenation |
| 收稿时间： | 2010-05-21 |
Novel Method for Selective Debenzylation Under Maintenance of Fluoro Atom Substituted on β-Amino Acids |
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| ZHENG Yi,WU Gang,ZHU Xin-rong,LI Yue-jie,MA Yu-heng,ZHAO Xin,LU Tao , ZHU Yong-qiang . School of Basic Sciences,China Pharmaceutical University,Nanjing ,P. R. China,. Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research,Jiangsu Simcere Pharmaceutical Research Institute,Nanjing. Novel Method for Selective Debenzylation Under Maintenance of Fluoro Atom Substituted on β-Amino Acids[J]. Chemical Research in Chinese University, 2011, 27(2): 224-227 |
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| Authors: | ZHENG Yi WU Gang ZHU Xin-rong LI Yue-jie MA Yu-heng ZHAO Xin LU Tao ZHU Yong-qiang . School of Basic Sciences China Pharmaceutical University Nanjing P. R. China . Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research Jiangsu Simcere Pharmaceutical Research Institute Nanjing |
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| Affiliation: | 1. School of Basic Sciences, China Pharmaceutical University, Nanjing 210009, P. R. China;
2. Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, Jiangsu Simcere Pharmaceutical Research Institute, Nanjing 210042, P. R. China |
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| Abstract: | tert-Butyl (R)-3-amino-3-(3-fluorophenyl)propanoate(5) was prepared with conventional debenzylation method. However, the tert-butyl (R)-3-[(S)-1-phenylethyl-amino]-3-(3-fluorophenyl) propanoate(6) and tert-butyl (R)-3-amino-3-phenylpropanoate(7) were generated as the byproducts under the general catalytic hydrogenation Pd(OH)2/C-H2 conditions. So a series of experiments was performed to optimize the reaction conditions so that product 5 could be obtained with high purity and yield. Finally an effective cata... |
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| Keywords: | β-Amino acid Debenzylation Defluorination Catalytic hydrogenation |
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