2-氯-6-苯胺基嘌呤衍生物的合成研究

Synthesis of 2-chloro-6-anilino-purine derivatives

N6嘌呤衍生物是重要的核苷类药物的中间体,以2,6-二氯嘌呤为原料,通过亲核取代反应合成2-氯-6-苯胺基嘌呤。研究了溶剂对反应的影响,以DMSO为溶剂,120℃搅拌反应10 h,产物收率52.2%。探讨了微波辐射对该反应的影响,研究了微波功率及照射时间对产物收率的影响。结果表明,微波辐射对该反应具有很好的促进作用,合适的反应条件为,微波功率300W照射10min,产物收率78.8%。产物结构经1H NMR表征。

N^6-purine derivatives were important Pharmaceutical intermediates of nucleotide. Considering the materials of 2, 6-dichloropurine, 2-chloro-6-anilino- purine was synthesized by nucleophilic.The effect of solvent on the reaction was studied. The reaction could be stirred for 10 h in DMSO, 120 ℃, with 52.2% yield. The effects of microwave power and irradiation time were explored. The results indicated that the reaction could be promoted by microwave radiation. The suitable reaction conditions of microwave irradiation were microwave irradiation 10 min with 300 W power. The yields were 78.8%. The products were confirmed by ^1H NMR characterization.