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【结 构 式】 
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【分子编号】44962 【品名】7-benzyl-2,6-dichloro-7H-purine 【CA登记号】 |
【 分 子 式 】C12H8Cl2N4 【 分 子 量 】279.12788 【元素组成】C 51.64% H 2.89% Cl 25.4% N 20.07% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(III)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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