| 骨髓增殖性肿瘤治疗药物TG101348的合成工艺研究 |
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| 引用本文： | 张义军,刘义稳,李德江. 骨髓增殖性肿瘤治疗药物TG101348的合成工艺研究[J]. 江西师范大学学报(自然科学版), 2014, 0(6): 635-638 |
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| 作者姓名： | 张义军 刘义稳 李德江 |
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| 作者单位： | 三峡大学生物与制药学院,湖北 宜昌,443002；三峡大学材料与化工学院,湖北 宜昌,443002 |
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| 基金项目： | 国家自然科学基金，湖北省自然科学基金 |
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| 摘 要： | 研究了骨髓增殖性肿瘤治疗药物TG101348的合成工艺.将2，4-二羟基-5-甲基嘧啶与三氯氧磷、氨水发生氯化、取代反应生成2-氯-4-氨基-5-甲基嘧啶（Ⅲ），而后Ⅲ与N-叔丁基-3-溴苯磺酰胺（Ⅰ）发生Buchwald偶联反应得到3-[（2-氯-5-甲基-4-嘧啶基）胺基]-N-（叔丁基）苯磺酰胺（Ⅳ），Ⅳ再与CH3 OH-HCl反应得到3-[（2-氯-5-甲基-4-嘧啶基）胺基]-N-（叔丁基）苯磺酰胺盐酸盐（Ⅴ），最后Ⅴ与1-（4-氨基苯氧乙基）吡咯烷（Ⅵ）发生亲核取代反应得到TG101348，HPLC测得TG101348的纯度为99.7；.
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| 关 键 词： | TG101348 合成 工艺研究 |
The Study on a Process of the Synthesis Bone Marrow Hyperplastic Tumortreatment Medicine TG101348 |
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| ZHANG Yi-jun,LIU Yi-wen,LI De-jiang. The Study on a Process of the Synthesis Bone Marrow Hyperplastic Tumortreatment Medicine TG101348[J]. Journal of Jiangxi Normal University (Natural Sciences Edition), 2014, 0(6): 635-638 |
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| Authors: | ZHANG Yi-jun LIU Yi-wen LI De-jiang |
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| Affiliation: | ZHANG Yi-jun;LIU Yi-wen;LI De-jiang;College of Biology and Pharmacy,China Three Gorges University;College of Materials and Chemical Engineering,China Three Gorges University; |
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| Abstract: | The synthetic technique of TG101348 for treating bone marrow hyperplastic tumor was studied. 2-chloro-4-amino-5-methyl-pyrimidine(Ⅲ)was prepared by chlorination and substitution reaction of 2 ,4-dihydroxy-5-meth-ylpyrimidinnel,phosphorus oxychloride and ammonium hydroxide.Ⅲreacted with 3-bromo-N-t-butyl benzenesulfon-ic amide(Ⅰ) to give 3-[( 2-chloro-5-methyl-4-pyrimidinyl ) amino ]-N-t-butyl benzenesulfonic amide(Ⅳ) by Buchwald coupling reaction.Ⅳ reacted with CH3 OH-HCl to afford 3-[(2-chloro-5-methyl-4-pyrimidinyl)amino]-N-tert-butyl benzenesuiphon amide hydrochloride(Ⅴ). TG101348 was synthesized by nucleophilic substitution re-action of the intermediate Ⅴ and Ⅵ. HPLC purity is 99 . 7；. |
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| Keywords: | TG101348 synthesis technical study |
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