| 含哌嗪基7-溴噻吩并[3,2-d]嘧啶抗癌试剂的设计与合成 |
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| 引用本文： | 蒋达洪,彭进松.含哌嗪基7-溴噻吩并[3,2-d]嘧啶抗癌试剂的设计与合成[J].化学研究与应用,2012(8):1247-1250. |
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| 作者姓名： | 蒋达洪 彭进松 |
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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;东北林业大学理学院 |
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| 基金项目： | 广东石油化工学院博士科研启动项目(2010b3)资助 |
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| 摘 要： | 为寻找以蛋白酪氨酸激酶为靶点的新型抗癌试剂,本文设计与合成了系列含哌嗪基的7-溴噻吩并3,2-d]嘧啶衍生物。以巯基乙酸为原料,经六步反应得4-氯-7-溴噻吩并3,2-d]嘧啶母核,再与不同的哌嗪衍生物在添加三乙胺作碱的条件下反应,制备了五个未见报道的含哌嗪基7-溴噻吩并3,2-d]嘧啶化合物。结构经1H NMR和HRMS表征。
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| 关 键 词： | 哌嗪 噻吩并[3 2-d]嘧啶 设计 抗癌试剂 |
Design and synthesis of 7-bromothieno[3,2-d]pyrimidine derivatives containing piperazine unit as anticancer agents |
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| JIANG Da-hong,PENG Jin-song.Design and synthesis of 7-bromothieno[3,2-d]pyrimidine derivatives containing piperazine unit as anticancer agents[J].Chemical Research and Application,2012(8):1247-1250. |
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| Authors: | JIANG Da-hong PENG Jin-song |
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| Institution: | 1.Department of Chemistry and Life Science,Guangdong University of Petrochemical Technology,Maoming 525000,China; 2.College of Science,Northeast Forestry University,Haerbin 150040,China) |
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| Abstract: | In the quest for novel protein tyrosine kinase inhibitors as putative anti-cancer agents,a series of 7-bromothieno3,2-d]pyrimidines containing a piperazine unit were designed and sgnthesized.Starting from mercaptoacetic acid,7-bromo-4-chlorothieno3,2-d]pyrimidine was obtained by 6-step reactions.Five novel 7-bromothieno3,2-d]pyrimidines containing a piperazine unit were synthesized through the reactions between the 7-bromo-4-chlorothieno3,2-d]pyrimidine and piperazine derivatives in the presence of Et3N.These new compounds were characterized with 1H NMR and HRMS. |
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| Keywords: | piperazine thieno[3 2-d]pyrimidine design anticancer agent |
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