培美曲塞二钠的合成 |
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引用本文: | 易必新,叶海,张鹏,张灿.培美曲塞二钠的合成[J].中国医药工业杂志,2006,37(12):798-800. |
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作者姓名: | 易必新 叶海 张鹏 张灿 |
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作者单位: | 中国药科大学新药研究中心,江苏,南京,210009 |
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摘 要: | 对碘苯甲酸甲酯与3-丁烯醇反应后溴代得4-(3-溴-4-氧代丁基)苯甲酸甲酯,与2,4-二氨基-6-羟基嘧啶反应后,再经水解得重要中间体2-氨基-4-氧代-5-2-(4-羧基苯基)乙基]-4,7-二氢-3H-吡咯并2,3-d]嘧啶,最后与L-谷氨酸二乙酯盐酸盐酰化、水解得培美曲塞二钠,总收率16%。
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关 键 词: | 培美曲塞 抗肿瘤药 抗叶酸剂 合成 |
文章编号: | 1001-8255(2006)12-0798-03 |
收稿时间: | 2006-03-17 |
修稿时间: | 2006-03-17 |
Synthesis of Pemetrexed Disodium |
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Authors: | YI Bi-Xin YE Hai ZHANG Peng ZHANG Can |
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Institution: | Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009 |
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Abstract: | Pemetrexed was synthesized from methyl 4-iodobenzoate to afford 4-(4-oxobutyl)benzoic acid methyl ester, which was subjected to bromination with isopropylidene dibromomalonate, and subsequent to cyclization with 2,4-diamino-6-hydroxyprimidine, hydrolysis to give 2-amino-4,7-dihydro-4-oxo-5-2-(4-carboxyphenyl)ethyl]- 1H-pyrrolo2,3-d]pyrimidine, followed by condensation with L-glutamic acid diester, and hydrolysis to give pemetrexed disodium in an overall yield 16%. |
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Keywords: | pemetrexed antimmor anfifolate synthesis |
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