2-氯-6-N-芳基取代嘌呤衍生物的合成

N6嘌呤衍生物是重要的核苷类药物的中间体.以2-氨基-6-氯嘌呤为原料,通过重氮化反应制得2,6-二氯嘌呤,收率30.5%.2,6-二氯嘌呤分别与苯胺、邻氯苯胺和对氯苯胺,通过N-烃基化反应制得2-氯-6-N-芳基嘌呤,收率75.2%;2-氯-6-N-2′-氯苯基嘌呤,收率68.5%和2-氯-6-N-4′-氯苯基嘌呤,收率63.2%.使用元素分析、核磁共振、质谱和红外光谱对所得产品进行分析,结果表明所得产品为目标产品.2-氯-6-N-芳基取代嘌呤衍生物合成的最佳工艺条件为：n（2,6-二氯嘌呤）∶n（苯胺衍生物）=1∶5,使用戊醇为反应中的溶剂,其用量为m（C5H11OH）∶m（2,6-二氯嘌呤）=23∶1,反应温度为80℃.

Synthesis of 2-chloro-6-N-aryl substituted purine derivatives

N^6-purine derivatives is a kind of important Pharmaceutical intermediates of nucleotide. Considering the materials of 2-amino-6-chloropurine , 2,6-dipchloropurine （yield 30.5 % ） was synthesized by diazotization. Through N-alkyl reaction, 2-chloro-6-N-arylpurine （ yield 75.2% ）, 2-chloro-6-N-2＇-chlorophenylpurine （yield 68.5% ） , 2-chloro-6-N-4＇-chlorophenylpurine （yield 63.2% ） was synthesized from the materials of 2,6-dipchloropurine and aniline, 2-chloro benzeneamine, and 4-chlorobenzeneamine. The products were analyzed by elemental analysis, ^1H NMR, MS and IR. Furthermore, 2-chloro-6-N-aryl substituted purine derivatives were studied particularly. The best craftwork are n （2-chloro-6-N-aryl） ： n （aniline-derivative） = 1 ： 5, m （C5 Hu OH） ：m （2-chloro-6-N-aryl） =23： 1, reaction temperature 80℃.