微波辐射下嘌呤C-2,6位衍生物及“Reversine”的合成

Microwave-Assisted Synthesis of the C-2,6 Derivatives of Purine and“Reversine”

以2,6-二氯嘌呤为原料,微波辐射法合成了"Reversine"[1,2-(4-吗啉苯胺基)-N6-环己基腺嘌呤]的重要中间体2-氯-6-环己胺基嘌呤及其衍生物3b～3f,再以2-氯-6-环己胺基嘌呤为原料,微波辐射下合成了2-苯胺基-6-环己胺基嘌呤及"Reversine"。探索了合适的反应条件及影响因素,产物的结构通过1 H NMR进行了表征。研究表明,微波法可大幅提高合成嘌呤2,6位衍生物收率并缩短反应时间,为嘌呤衍生物及"Reversine"的合成提供了一种绿色、简洁高效的合成方法。

A practical synthesis of 2-chloro-6-cyclohexylaminopurine, an important intermediate of ＂Reversine＂ [-1, 2-（4-morpholinoanilino）-N6-cyclohexyladenine] and its derivatives 3b - 3f, was described starting from 2,6-dichloropurine by microwave irradiation. ＂Reversine＂ and the compound of 2-phenylamino-6-cyclohexylamino purine were synthesized from 2-chloro-6-cyclohexylaminopurine under microwave irradiation successfully. Main factors affecting conversion of such reactions was investigated. The structures of the target compounds 3a~ 3f, 4 and I were characterized by ^1H NMR. The results indicated that the C- 2, 6 derivatives of purine and ＂Reversine＂ were rapidly synthesized with high yields. Microwave irradia- tion, a method of high efficiency and environment benefit could be used in the synthesis of purine derivatives and ＂Reversine＂.