| 含哌嗪基噻吩并[3,2-d]嘧啶类抗癌试剂的设计与合成 |
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| 引用本文： | 蒋达洪,黄敏. 含哌嗪基噻吩并[3,2-d]嘧啶类抗癌试剂的设计与合成[J]. 化学试剂, 2012, 34(9): 797-799,806 |
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| 作者姓名： | 蒋达洪 黄敏 |
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| 作者单位： | 广东石油化工学院化学与生命科学学院,广东茂名,525000 |
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| 基金项目： | 广东石油化工学院博士科研启动项目 |
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| 摘 要： | 基于蛋白酪氨酸激酶为靶点的抗癌试剂的结构特点,设计与合成了系列含哌嗪基的噻吩并[3,2-d]嘧啶衍生物。以巯基乙酸为原料,经酯化、两次缩合成环、氯代等4步反应得4-氯噻吩并[3,2-d]嘧啶母核,再与不同的哌嗪衍生物在DMF中发生亲核取代反应,制备了4个未见报道的含哌嗪基噻吩并[3,2-d]嘧啶化合物,产物结构经1HNMR和HRMS表征。
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| 关 键 词： | 哌嗪 噻吩并[3,2-d]嘧啶 抗癌试剂 设计 合成 |
Design and synthesis of thieno [ 3,2-d ] pyrimidine derivatives containing a piperazine unit as anticancer agents |
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| JIANG Da-hong , HUANG Min. Design and synthesis of thieno [ 3,2-d ] pyrimidine derivatives containing a piperazine unit as anticancer agents[J]. Chemical Reagents, 2012, 34(9): 797-799,806 |
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| Authors: | JIANG Da-hong HUANG Min |
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| Affiliation: | (Department of Chemistry and Life Science,Guangdong University of Petrochemical Technology,Maoming 525000,China) |
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| Abstract: | A series of thieno[3,2-d]pyrimidines incorporated with a piperazine unit as putative anti-cancer agents were designed and synthesized based on the structure of protein tyrosine kinase inhibitors.Starting from mercaptoacetic acid,4-chlorothieno[3,2-d]pyrimidine was obtained by 4-step reactions through esterification,twice ring closure condensations,and substitution with chlorine.Four novel thieno[3,2-d]pyrimidines containing a piperazine unit were synthesized through the reactions of 4-chlorothieno[3,2-d]pyrimidine with piperazine derivatives in DMF.The structures were confirmed with1HNMR and HRMS. |
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| Keywords: | piperazine thieno[3,2-d]pyrimidine anticancer agent design synthesis |
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