| 犬尿氨酸羟化酶选择性抑制剂L-3-(邻甲氧基苯甲酰基)丙氨酸的简捷合成 |
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| 引用本文： | 马向东,姚祝军. 犬尿氨酸羟化酶选择性抑制剂L-3-(邻甲氧基苯甲酰基)丙氨酸的简捷合成[J]. 化学学报, 2006, 64(21): 2197-2200 |
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| 作者姓名： | 马向东 姚祝军 |
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| 作者单位： | 中国科学院上海有机化学研究所,生命有机化学国家重点实验室,上海,200032 |
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| 摘 要： | 从Boc-保护氨基的天冬氨酸苄酯出发, 通过5步反应简捷地合成了犬尿氨酸羟化酶的选择性抑制剂L-3-(邻甲氧基苯甲酰基)丙氨酸(o-MBA). 其中关键反应为锂试剂对Weinreb酰胺的亲核取代反应.
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| 关 键 词： | L-3-(邻甲氧基苯甲酰基)丙氨酸 Weinreb酰胺 芳基锂试剂 犬尿氨酸酶 抑制剂 |
| 收稿时间： | 2006-04-25 |
| 修稿时间： | 2006-04-25 |
A Concise Synthesis of L-3-(o-Methoxybenzoyl)alanine, a Selective Kynurenine Hydroxylase Inhibitor |
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| MA,Xiang-Dong,YAO,Zhu-Jun. A Concise Synthesis of L-3-(o-Methoxybenzoyl)alanine, a Selective Kynurenine Hydroxylase Inhibitor[J]. Acta Chimica Sinica, 2006, 64(21): 2197-2200 |
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| Authors: | MA Xiang-Dong YAO Zhu-Jun |
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| Affiliation: | (State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032) |
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| Abstract: | A concise five-step synthesis of L-3-(o-methoxybenzoyl)alanine, a selective kynurenine hy- droxylase inhibitor is described starting from commercially available 4-benzyl L-N-(tert-butoxycarbonyl) aspartate. Aryl lithium addition to the corresponding Weinreb amide successfully served as the key step. |
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| Keywords: | L-3-(o-methoxybenzoyl)alanine Weinreb amide aryl lithium kynurenine hydroxylase inhibi- tor |
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