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以尿苷(1a)或2’-脱氧尿苷(1b)类化合物为原料,经碘代、选择性氧化、Heck反应等步骤快捷、环保地合成(E)-5-(2-溴乙烯基)尿苷/(E)-5-(2-溴乙烯基)-2’-脱氧尿苷(5a/5b),再通过酯化、硫羰基化、氨解等步骤合成新化合物(E)-4-硫-5-(2-溴乙烯基)尿苷/(E)-4-硫-5-(2-溴乙烯基)-2’-脱氧尿苷(8a/8b),共得到5种新的硫代产物,其中包含2种新产物8a/8b,3种新中间体7a,7b,10.其结构通过~1H NMR,~(13)C NMR,IR,UV,HRMS,X-Ray等谱图手段进行了表征.采用3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2H-溴化四唑(MTT)实验方法对8a及其类似物进行了细胞毒性评价,发现8a/8b是潜在的抗肿瘤药物.
Using uridine (1a) or 2’-deoxyuridine (1b) as starting material, the (E) -5- (2-bromovinyl (E) -5- (2-bromovinyl) -2’-deoxyuridine (5a / 5b) is synthesized by the esterification, thiocarbonylation, 5 (2-bromovinyl) uridine and (E) -4-thio-5- (2-bromovinyl) -2’-deoxyuridine (8a / 8b) The new thio-products, which contain two new products, 8a / 8b, and three new intermediates, 7a, 7b and 10, were identified by 1H NMR, 13 C NMR, IR, UV, HRMS, Isopiperazine was used to characterize 8a and its analogues by the method of 3- (4,5-dimethyl-2-thiazolyl) -2,5-diphenyl-2H-tetrazolium tetrazolium (MTT) The cytotoxicity was evaluated and 8a / 8b was found to be a potential anti-tumor drug.