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📜甲酸环己酯置于劳森试剂体系中,用 乙醚 用作溶剂,化学反应 0.01H,反应生成杀螨醚
参考文献:将过量的芳基-格利雅试剂和亲电试剂顺序单罐添加到邻烷基硫代甲酸酯中
标题:将过量的芳基-格利雅试剂和亲电试剂顺序单罐添加到邻烷基硫代甲酸酯中
摘要:将芳族格氏试剂顺序添加到o-烷基硫代甲酸酯中可在30 S内完成,以高收率得到芳基苄基硫烷.该反应可能始于格氏试剂对o-烷基硫代甲酸酯的碳原子的亲核攻击,然后消除romgbr生成芳族硫醛,然后与格氏试剂的第二个分子在硫原子处反应生成形成芳基硫烷基苄基格氏试剂.为了确认芳族硫醛的产生,O之间的反应烷基硫代甲酸酯和苯基格氏试剂是在环戊二烯存在下进行的.结果,形成了硫代醛和二烯的杂diels-Alder加合物.硫代甲酸酯和苯基格氏试剂与碘的混合物处理后得到1,2-双(苯基硫烷基)-1,2-二苯基乙烷产物,表明在反应混合物中形成了芳基硫烷基苄基格氏试剂.当将亲电试剂添加到原位生成的格利雅试剂中时,四组分偶联产物即o烷基硫甲酸酯,格氏试剂的两个分子和亲电试剂以中等至非常好的收率获得.使用甲硅烷基氯或烯丙基溴化物可在5分钟内得到加合物,而与苄基卤化物的反应则需要30分钟以上.在1分钟内即可完成向羰基化合物
Doi:10.1002/chem.201301573

专利信息

专利号:WO-2025056767-A1
优先权日:2023-09-15
标题 :Process for the preparation of enantiomerically enriched aliphatic amines
发明人：BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS
权利人:SYNGENTA CROP PROTECTION AG
摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.

专利号:US-5717099-A
优先权日:1994-03-28
标 题:Method of synthesis for 6,9-bis((2-aminoethyl)amino)benzo g!isoquinoline-5,10-dione and its dimaleate salt
发明人：SPINELLI SILVANO; DIDOMENICO ROBERTO
权利人:BOEHRINGER MANNHEIM ITALIA
摘要:In the search for novel heteroanalogs of anthracendiones, 6,9-bis (2-aminoethyl)amino!benzo g!isoquinoline-5,10-dione dimaleate salt (BBR 2778), was selected as the most promising compound. New methods of synthesis produce the compound in purity greater than 99%.

专利号:WO-2021074309-A1
优先权日:2019-10-16
标 题:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives as fungicides for combating specific phytopathogens
发明人：WEISS MATTHIAS; QUARANTA LAURA; BOU HAMDAN FARHAN; MAHAJAN ATUL; WILLIAMS SIMON; KILARU JAGADEESH; SEN INDIRA; BIERI STEPHANE; DIGGELMANN MARTIN
权利人:SYNGENTA CROP PROTECTION AG
摘要:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives of formula (I) as well as a method of combating, preventing or controlling the phytopathogens Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale), which comprises applying to the phytopathogen, to the locus of the phytopathogen, or to a plant susceptible to attack by the phytopathogen, or to propagation material thereof, a fungicidally effective amount of a 1-(3-quinolyl)-3,4-dihydroisoquinoline derivative of formula (I). The present description discloses the synthesis of exemplary compounds, formulation examples, relevant biological data (antifungal activity against Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale) when spayed on plants), as well as comparative data against three prior art compounds (e.g. pages 52 to 85; formulation examples; examples A1 to A3; table E; compounds E.01 to E.187; biological examples). Exemplary compounds are e.g.: 5-bromo-1-(8-fluoro-3-quinolyl)spiro[4H-isoquinoline-3,1'- cyclopropane] (example A1) 5-bromo-1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline (example A2) 1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline-5-carbonitrile (example A3)

专利号:WO-2021074311-A1
优先权日:2019-10-16
标题:1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives as fungicides for combating specific phytopathogens
发明人：WEISS MATTHIAS; QUARANTA LAURA; BOU HAMDAN FARHAN; MAHAJAN ATUL; WILLIAMS SIMON; KILARU JAGADEESH; BIERI STEPHANE; DIGGELMANN MARTIN
权利人:SYNGENTA CROP PROTECTION AG
摘要:1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) as well as a method of combating, preventing or controlling the phytopathogens Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale), which comprises applying to the phytopathogen, to the locus of the phytopathogen, or to a plant susceptible to attack by the phytopathogen, or to propagation material thereof, a fungicidally effective amount of a 1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives of formula (I). The present description discloses the synthesis of exemplary compounds, formulation examples, relevant biological data (antifungal activity against Mycosphaerella graminicola, Monographella nivalis, Fusarium culmorum and/or Gibberella zeae when spayed on plants) (e.g. pages 47 to 55; examples A1 and A2; compounds E.01 to E.17; table E). An exemplary compounds is e.g.: 3-(5-bromo-3,3-dimethyl-2,4-dihydro-1 H-isoquinolin-1-yl)-8-fluoro- quinoline (example A1)

专利号:RU-2144028-C1
优先权日:1994-03-28
标题:Improved methods of synthesis of 6,9-bis-[(2-aminoethyl)- -amino]benzo[g]isoquinoline-5,10-dione maleate

专利号:CZ-284937-B6
优先权日:1994-03-28
标 题:Improved method for the synthesis of 6,9-bis [(2-aminoethyl) amino] benzo [g] isoquinoline-5,10-dione and its dimaleate salt