Synthesis of 1-substituted-3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine
The synthesis of a class of 1-substituted-3-iodo-1H-pyrazolo[3,4-d]pyrimidine-4-amines(1a～1e)was reported.The N-alkylation reaction of 3-iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine(2)with iodoethane(3a),iodomethane(3b),2-iodopropane(3c),iodocyclobutane(3d)and iodocyclopentane(3e)was studied respectively,five kinds of 1-substituted-3-iodo-1H-pyrazolo[3,4-d]pyrimidine-4-amines(1a～1e)were obtained.And their structures were confirmed by 1H NMR and ESI-MS.The optimum conditions for N-alkylation were as follows:the mole ratio n(3a)∶n(2)=4∶1,N,N-dimethylformamide as solvent,cesium carbonate as base,and the reaction temperature was 110℃.
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