[1]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,(06):635-638.
 ZHANG Yi-jun,LIU Yi-wen,LI De-jiang.The Study on a Process of the Synthesis Bone Marrow Hyperplastic Tumortreatment Medicine TG101348[J].,2014,(06):635-638.
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骨髓增殖性肿瘤治疗药物TG101348的合成工艺研究()
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《江西师范大学学报》(自然科学版)[ISSN:1006-6977/CN:61-1281/TN]

卷:
期数:
2014年06期
页码:
635-638
栏目:
出版日期:
2014-12-31

文章信息/Info

Title:
The Study on a Process of the Synthesis Bone Marrow Hyperplastic Tumortreatment Medicine TG101348
作者:
张义军;刘义稳;李德江
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
Author(s):
ZHANG Yi-jun;LIU Yi-wen;LI De-jiang
关键词:
TG101348合成工艺研究
Keywords:
TG101348synthesistechnical study
分类号:
TQ463.53
文献标志码:
A
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;.
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;.

参考文献/References:

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备注/Memo

备注/Memo:
国家自然科学基金(31100080);湖北省自然科学基金(2011CDB186)
更新日期/Last Update: 1900-01-01