专利号:US-4152517-A 优先权日:1977-10-19 标题:Synthesis of 6-(2-hydroxyphenyl)-3(2H)-pyridazinones from trihalocarbinols 发明人:LEVINSON SIDNEY H; MENDELSON WILFORD L 权利人:SMITHKLINE CORP 摘要:A new synthesis for the preparation of 6-(2-hydroxyphenyl)-3-pyridazinones whose key reaction is cyclizing a 1,1,1-trihalo-2-hydroxy-4-(2-hydroxyphenyl)-1-butanone with hydrazine. 6-(2-Hydroxyphenyl)-3-pyridazinones are important intermediates for preparing medicinally active compounds.
专利号:US-4193941-A 优先权日:1977-10-19 标 题:1,1,1-Trihalo-2-hydroxy-4-(2-hydroxyphenyl)-4-butanones 发明人:LEVINSON SIDNEY H; MENDELSON WILFORD L 权利人:SMITHKLINE CORP 摘要:A new synthesis for the preparation of 6-(2-hydrophenyl)-3-pyridazinones whose key reaction is cyclizing a 1,1,1-trihalo-2-hydroxy-4-(2-hydroxyphenyl)-4-butanone with hydrazine. 6-(2-Hydroxyphenyl)-3-pyridazinones are important intermediates for preparing medicinally active compounds especially 3-[2-(3-tert.-butylamino-2-hydroxypropoxy)phenyl]-6-hydrazinopyridazine or its nontoxic acid addition salts. The invention claimed here is the trihalocarbinol intermediates.
参考标题:One-Pot Preparation Of 6-Substituted 3(2H)-Pyridazinones From Ketones 作者:W. J. Coates,A. Mckillop 摘要:A One-Pot Process For The Preparation Of 6-Phenyl-3(2H)-Pyridazinone From Acetophenone And Glyoxylic Acid Has Been Investigated And Shown To Have Wide Utility In The Preparation Of 6- And 5,6-Substituted 3(2H)-Pyridazinones. Limitations To The Process Encountered With 2′-Hydroxyacetophenone And With Basic Heteroaromatic Ketones Have Been Overcome, And The Processes Described Offer The Rapid And Efficient Synthesis Of Many 6-Substituted Pyridazinones From Readily Available Ketones.
合成参考文献
参考文献:10.1016/j.ejmech.2021.114098 摘要:Shi Y, Zhang H, Song Q, Yu G, Liu Z, Zhong F, Tan Z, Liu X, Deng Y. Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. European Journal of Medicinal Chemistry. 2022 Feb;230():114098. doi: 10.1016/j.ejmech.2021.114098. 摘要:Haider, N.; Holzer, W., Science of Synthesis, (2004) 16, 187. 摘要:Haider, N.; Holzer, W., Science of Synthesis, (2004) 16, 134.