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5-氯-6-苯基-2H-哒嗪-3-酮的合成 被引量:1

Synthesis of 5-Chloro-6-phenyl-2H-pyridazin-3-one
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摘要 6-苯基-2H-哒嗪-3-酮(2)经三氯化磷/氯气氯代制得3,5-二氯-6-苯基哒嗪,经氢氧化钠皂化,再用盐酸调至pH 8.5得到5-氯-6-苯基-2H-哒嗪-3-酮,总收率约24%(以2计)。副产物3-氯-5-羟基-6-苯基哒嗪可作为氯代反应的原料回收使用。 5-Chloro-6-phenyl-2H-pyridazin-3-one was synthesized from 6-phenyl-2H-pyridazin-3-one (2) by chlorination with phosphorus trichloride and chlorine to give 3,5-dichloro-6-phenylpyridazine, which was saponified with sodium hydroxide, followed by acidification with hydrochloric acid to pH 8.5 with an overall yield of about 24% (based on compound 2). The by-product 3-chloro-5-hydroxy-6-phenylpyridazine from saponification can be reused as raw material in chlorination.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2010年第11期803-804,共2页 Chinese Journal of Pharmaceuticals
基金 国家自然科学基金资助项目(50773009) 上海市科委基金资助项目(08JC1400600) 中央高校专项基金和教育部博士点新教师基金(2009007512001) 2010大学生创新课题(CX2010-17)
关键词 5-氯-6-苯基-2H-哒嗪-3-酮 3-氯-5-羟基-6-苯基哒嗪 中间体 合成 5-chloro-6-phenyl-2H-pyridazin-3-one 3-chloro-5-hydroxy-6-phenyllpyridazine intermediate synthesis
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  • 1Coelho A, Sotelo E, Fraiz N, et al. Pyridazines. Part 36: Synthesis and antiplatelet activity of 5-substituted-6-phenyl- 3 (2//) -pyridazinones [J]. Bioorg Med Chem Lett, 2004, 14(2) : 321-324.
  • 2Sotelo E, Fraiz N, Yanez M, et al. Pyridazines. Part 28: 5-Alkylidene-6-phenyl-3 (2H) -pyridazinones, a new family of platelet aggregation inhibitors [J]. Bioorg Med Chem Lett, 2002, 12 (12) : 1575-1577.
  • 3Ravina E, Teran C, Santana L, et al. Piridazine derivatives. IX. Synthesis of 2H-pyridazin-3-ones with aroylpiperazinyl groups [J]. Heteroeyeles, 1990, 31 (11): 1967-1974.
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