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Synthesis of 2-chloro-4-(3-nitrophenoxy) thieno [3, 2-d] pyrimidine
IOP Conference Series: Earth and Environmental Science Pub Date : 2019-07-09 , DOI: 10.1088/1755-1315/252/2/022091
Zhihui Zhou , Caolin Wang , Zhen Xiao , Qi Yang , Shan Xu

2, 4-dichloro-6-(3-nitrophenoxy) pyrimidine is an important intermediate of small molecule anticancer drugs. In this work, a rapid synthetic method for target compounds was established. Compound (4) was synthesized from methyl 3-aminothiophene-2-carboxylate and urea through three steps including cyclization, chlorination and nucleophilic substitution. The structure of the target compound was confirmed by 1H NMR and MS spectrum. Furthermore, the synthetic method was optimized. The total yield of the three steps was 42.4%.

中文翻译:

2-氯-4-(3-硝基苯氧基)噻吩并[3, 2-d]嘧啶的合成

2、4-二氯-6-(3-硝基苯氧基)嘧啶是小分子抗癌药物的重要中间体。在这项工作中,建立了一种目标化合物的快速合成方法。化合物(4)由3-氨基噻吩-2-羧酸甲酯和尿素通过环化、氯化和亲核取代三个步骤合成。目标化合物的结构经1H NMR和MS谱证实。此外,还对合成方法进行了优化。三步总收率为42.4%。
更新日期:2019-07-09
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