| 叶酸拮抗剂Alimta的合成 |
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| 引用本文： | 郭志雄,王荷芳,辛春伟,陈立功. 叶酸拮抗剂Alimta的合成[J]. 有机化学, 2006, 26(4): 546-550 |
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| 作者姓名： | 郭志雄 王荷芳 辛春伟 陈立功 |
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| 作者单位： | 1. 天津大学药物与科学技术学院,天津,300072
2. 天津大学化工学院,天津,300072 |
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| 摘 要： | 吡咯并[2,3-d]嘧啶类叶酸拮抗剂Alimta (1)是一种多靶向的抗癌药物, 本工作建立了新的方法全合成该药物. 通过Friedel-Crafts反应、黄鸣龙反应制备了4-(4-乙氧基-4-氧正丁基)苯甲酸乙酯(5), 收率为36.6%. 然后采用KBH4/LiBr对5选择性还原, 再经氧化、成环等反应最终合成该药. 总收率4.8%.
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| 关 键 词： | 吡咯并[2,3-d]嘧啶 叶酸拮抗剂 Alimta Friedel-Crafts反应 黄鸣龙反应 |
| 收稿时间： | 2005-03-14 |
| 修稿时间： | 2005-09-01 |
Synthesis of Antifolate Alimta |
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| GUO,Zhi-Xiong,WANG,He-Fang,XIN,Chun-Wei,CHEN,Li-Gong. Synthesis of Antifolate Alimta[J]. Chinese Journal of Organic Chemistry, 2006, 26(4): 546-550 |
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| Authors: | GUO Zhi-Xiong WANG He-Fang XIN Chun-Wei CHEN Li-Gong |
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| Affiliation: | 1. School of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin 300072;2. School of Chemical Engineering, Tianjin University, Tianjin 300072 |
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| Abstract: | Antifolate alimta (1) derived from pyrrolo[2,3-d]pyrimidine is a multitargeted antitumor agent and a novel synthetic route to it was established. Ethyl 4-(4-ethoxy-4-oxobutyl)benzoate (5) was prepared via Friedel-Crafts acylation and Huang reduction in 36.6% yield, then alimta was synthesized through selec- tive reduction with KBH4/LiBr, oxidation, ring-closing and etc. in overall yield of 4.8%. |
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| Keywords: | pyrrolo[2 3-d]pyrimidine antifolate alimta Friedel-Crafts Huang reduction. |
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