3-炔基咪唑并[1,2-b]哒嗪的简便合成 |
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引用本文: | 唐武,王鹏旭,金波,林紫云,李刚,马辰,黄海洪. 3-炔基咪唑并[1,2-b]哒嗪的简便合成[J]. 合成化学, 2016, 0(7): 643-646. DOI: 10.15952/j.cnki.cjsc.1005-1511.2016.07.16109 |
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作者姓名: | 唐武 王鹏旭 金波 林紫云 李刚 马辰 黄海洪 |
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作者单位: | 中国医学科学院北京协和医学院药物研究所活性物质发现与适药化北京市重点实验室,北京,100050 |
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基金项目: | 中央公益性科研院所基本科研业务费(2016CX04) |
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摘 要: | 以咪唑并[1,2-b]哒嗪为原料,与N-碘代丁二酰亚胺在三氟乙酸/二氯甲烷中于室温进行碘代反应制得3-碘咪唑并[1,2-b]哒嗪(3);3与三甲基硅基乙炔在Pd(OAc)_2催化下经Sonogashira偶联反应制得3-三甲基硅基乙炔基咪唑并[1,2-b]哒嗪(4);4在碳酸钾作用下脱除三甲基硅基合成了3-炔基咪唑并[1,2-b]哒嗪,总收率61.2%,其结构经~1H NMR和HR-MS确证。
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关 键 词: | 3-炔基咪唑并1,2-b哒嗪 碘代反应 Sonogashira偶联 药物合成 |
Concise Synthesis of 3-Ethynylimidazo[1,2-b] pyridazine |
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Abstract: | 3-Iodoimidazo[1,2-b]pyridazine(3) was synthesized by iodination of imidazo [1,2-b]pyr-idazine with N-iodosuccinimide in the mixture of TFA and DCM .3-[ ( Trimethylsilyl ) ethynyl ] imidazo [1,2-b]pyridazine(4) was prepared by Sonogashira coupling reaction of 3 with trimethylsilylacetylene catalyzed by Pd(OAc)2.3-Ethynylimidazo[1,2-b]pyridazine with the total yield of 61.2%was synthe-sized by removal of trimethylsilyl of 4 in the presence of K 2 CO3 .The structure was confirmed by 1 H NMR and HR-MS . |
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Keywords: | 3-ethynylimidazo[1,2-b]pyridazine iodination Sonogashira coupling reaction drug synthesis |
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