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李天舒

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供职机构:北京大学基础医学院天然药物及仿生药物国家重点实验室更多>>
发文基金:国家自然科学基金更多>>
相关领域:医药卫生更多>>

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A new strategy for the synthesis of 3-deazaneplanocin A
2010年
3-Deazaneplanocin A (3-DNPA, 2), an antiviral and antitumor agent, has been synthesized in an optimized procedure in 10 steps, with an increased overall yield of 11.2%. Started from 2,4-dihyroxyl-3-nitropyridine, reduction of nitro group and ring closure of imidazole were carried out in one pot, without the separation of diaminopyridine (10), to give 3-deazapurine (11). Moreover, the conversion of 6-chloro-3-deazapurine (12) to 6-amino-3-deazapurine (13) and the synthesis of N^6,N^6,N9-tris-Boc-3- deazadenine (16) was promoted by microwave-aid method. Compound 16 benefited the formation of N9 isomer of 3-DNPA in Mitsunobu reaction.
李天舒陆世芳邢磊林桂椿关注杨振军
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