8-R-9苄基-9H-嘌呤衍生物的合成研究

Synthesis of 8-R-9-Benzyl-9H-purines

采用 (Ph3 P) 2 PdCl2 为催化剂 ,DMF为溶剂 ,对 8 碘 9 苄基 9H 嘌呤与有机锡试剂RSnBu3 (R=乙烯基、2 噻吩基、2 呋喃基、苯乙炔基和苯基等 )之间的Stille偶合反应进行了研究 ,合成出了5种 8位取代的嘌呤衍生物。在反应温度为 80℃ ,n(8 碘 9 苄基 9H 嘌呤 )∶n (RSnBu3 )∶n〔(Ph3 P) 2 PdCl2 〕 =1 0∶1 2∶0 0 5的较佳工艺条件下 ,产品收率 4 1%～ 91%。用1H NMR、13 C

The Stille coupling reaction between 8 iodo 9 benzyl 9H purine and RSnBu 3 (R=vinyl,2 thienyl,2 furyl,phenylethynyl and phenyl) was studied using (Ph 3P) 2PdCl 2 as catalyst and DMF as solvent.The optimum reaction conditions were reaction temperature 80 ℃ and n (8 iodo 9 benzyl 9H purine)∶ n (RSnBu 3)∶ n 〔(Ph 3P) 2PdCl 2)=1 0∶1 2∶0 05.Yields of the products were 41%-91%.The products were characterized by 1H NMR , 13 C-NMR and MS.