盐酸诺拉曲塞的合成 |
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引用本文: | 张庆文,郑云满,益兵,时惠麟.盐酸诺拉曲塞的合成[J].中国医药工业杂志,2008,39(11). |
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作者姓名: | 张庆文 郑云满 益兵 时惠麟 |
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作者单位: | 上海医药工业研究院,上海,200437 |
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基金项目: | 上海市科学技术委员会重人科技攻关项目 |
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摘 要: | 2-溴-4-硝基甲苯经催化氢化、与水合氯醛和盐酸羟胺反应、环合制得4-溴-5-甲基靛红,再经Baeyer-Villiger反应、甲酯化、与盐酸氯甲脒环合、Ullmann反应、成盐结晶制得胸苷酸合成酶抑制剂盐酸诺拉曲塞二水合物,总收率为8%。
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关 键 词: | 盐酸诺拉曲塞 胸苷酸合成酶抑制剂 抗肿瘤药 合成 多晶型 |
Synthesis of Nolatrexed Dihydrochloride |
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Authors: | ZHANG Qingwen ZHENG Yunman YI Bing SHI Huilin |
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Abstract: | Nolatrexed dihydrochloride dihydrate,a thymidylate synthase inhibitor,was synthesized from 2-bromo-4-nitrotoluene in 8%overall yield via catalytic hydrogenation,reaction with chloral hydrate and hydroxylamine hydrochloride,and cyclization to give 4-bromo-5-methylisatin,which was then subjected to Baeyer-Villiger reaction, esterification,cyclization with chloroformamidine hydrochloride,Ullmann reaction,and salt formation. |
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Keywords: | nolatrexed dihydrochloride thymidylate synthase inhibitor antitumor agent synthesis polymorphism |
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