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3-炔基咪唑并[1,2-b]哒嗪的简便合成 被引量:3

Concise Synthesis of 3-Ethynylimidazo[1,2-b]pyridazine
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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。 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 K2 CO2+. The structure was confirmed by 1H NMR and HR-MS.
出处 《合成化学》 CAS CSCD 2016年第7期643-646,共4页 Chinese Journal of Synthetic Chemistry
基金 中央公益性科研院所基本科研业务费(2016CX04)
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 3-ethynylimidazo [ 1,2-b ] pyridazine iodination Sonogashira coupling reaction drug synthesis
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