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目的合成作为肿瘤增敏剂和荧光探针分子连结子的新化合物O6-(对-羧基苄基)鸟嘌呤。方法以2-氨基-6-氯嘌呤(ACP)为起始原料,与三乙烯二胺(DABCO)反应生成DABCO-嘌呤,再进行亲核取代反应得到O6-(对-氰基苄基)鸟嘌呤这一重要中间体,最后将氰基水解为羧酸制得O6-(对-羧基苄基)鸟嘌呤。结果与结论合成获得了新结构化合物O6-(对-羧基苄基)鸟嘌呤,其结构经1H-NMR、LC-MS、13C-NMR谱得到确证,总收率为61.4%。重要中间体O6-(对-氰基苄基)鸟嘌呤的制备工艺得到优化,新工艺原料经济易得、操作简单,原子经济效率高、杂质少且易于纯化,适合工业化大生产。
OBJECTIVE: To synthesize O6- (p-carboxybenzyl) guanine, a neoplasm sensitizer and fluorescent probe molecule linker. Methods 2-Amino-6-chloropurine (ACP) was used as a starting material to react with triethylenediamine (DABCO) to form DABCO-purine, followed by nucleophilic substitution to obtain O6- (p- cyanobenzyl) Purine this important intermediate, and finally the hydrolysis of cyano to carboxylic acid O6- (p - carboxybenzyl) guanine. Results and Conclusion The new compound O6- (p-carboxybenzyl) guanine was synthesized and its structure was confirmed by 1H-NMR, LC-MS and 13C-NMR. The overall yield was 61.4%. The preparation process of O6- (p-cyanobenzyl) guanine, an important intermediate, has been optimized. The raw materials of the new process are easily available, simple in operation, economical in atomic economy, less impurities and easy to purify, and are suitable for industrialized large-scale production.