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| 培美曲塞二钠的合成研究进展 | |
| 引用本文： | 张静,范继业,程艳坤,黄永茂,高冬婷,陈.培美曲塞二钠的合成研究进展[J].河北化工,2009,32(5):5-6. |
| 作者姓名： | 张静 范继业 程艳坤 黄永茂 高冬婷 陈 |
| 作者单位： | 1. 河北化工医药职业技术学院,河北,石家庄,050026;河北科技大学化学与制药工程学院,河北,石家庄,050018 2. 河北化工医药职业技术学院,河北,石家庄,050026 3. 石家庄制药集团中诺药业有限公司,河北,石家庄,050000 |
| 摘 要： | 介绍了合成新型抗癌药物培美曲塞二钠的两种方法。一种是以对溴苯甲酸为起始原料经酯化、缩合、溴代、环合、成盐等反应合成目标化合物，总收率达13．9％。另一是对碘苯甲酸甲酯与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，总收率为16％。 |
| 关 键 词： | 培美曲塞二钠 抗肿瘤药 化学合成 |
Advances in Synthesis of Pemetrexed Disodium |
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| ZHANG Jing,FAN Ji-ye,CHENG Yan-kun,HUANG Yong-mao,GAO Dong-ting,CHEN Ying.Advances in Synthesis of Pemetrexed Disodium[J].Hebei Chemical Engineering and Industry,2009,32(5):5-6. | |
| Authors: | ZHANG Jing FAN Ji-ye CHENG Yan-kun HUANG Yong-mao GAO Dong-ting CHEN Ying |
| Affiliation: | ZHANG Jing,FAN Ji-ye, CHENG Yan-kun, HUANG Yong-mao,GAO Dong-ting , CHEN Ying (1. Hebei Chemical and Pharmaceutical Vocational Technology College, Shijiazhuang 050026, China;2. College of Chemical and Pharmaceutical Engineering ,Hebei University of Science and Technology, Shijiazhuang 050018, China;3. CSPC Zhongnuo Pharmaceutical(Shijiazhuang)Co., Ltd, Shijiazhuang 050000, China) |
| Abstract: | There are two methods which to synthesize pemetrexed disodium, a novel anti-cancerogenic drug. Pemetrexed disodium was prepared via esterification, condensation, bromination, cyclization reaction and so on. The overall yield was 13.9%. The other method is Pemetrexed that 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, hydroly... |
| Keywords: | pemetrexed disodium anticancer agent chemical synthesis |
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