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【结 构 式】 
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【药物名称】 【化学名称】9-Benzyl-2-chloro-6-(2-furyl)-9H-purine 【CA登记号】176515-43-8 【 分 子 式 】C16H11ClN4O 【 分 子 量 】310.74527 |
【开发单位】Universitetet i Oslo (Originator) 【药理作用】ANTIINFECTIVE THERAPY, Antimycobacterial Agents, Treatment of Tuberculosis |
合成路线1
2,6-Dichloropurine (I) was N-alkylated with benzyl chloride to give a 7:3 mixture of 9-benzyl-2,6-dichloropurine (II) and the 7-benzylated isomer (III). After chromatographic isolation of the desired 9-benzyl purine (II), Stille coupling with the 2-furyltin reagent (IV) in the presence of palladium catalyst furnished the corresponding 6-furylpurine.
| 【1】 Nissen-Meyer, J.; Spilsberg, B.; Gundersen, L.-L.; Synthesis and antimycobacterial activity of 6-arylpurines: The requirements for the N-9 substituent in active antimycobacterial purines. J Med Chem 2002, 45, 6, 1383. |
| 【2】 Langli, G.; et al.; Regiochemistry in Stille couplings of 2,6-dihalopurines. Tetrahedron 1996, 52, 15, 5625. |
| 【3】 Nolsoe, J.M.J.; Langli, F.; Bakkestuen, A.K.; Gundersen, L.-L.; 9-Benzylpurines with inhibitory activity against Mycobacterium tuberculosis. Bioorg Med Chem Lett 2000, 10, 11, 1207. |
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