专利号:US-2016073631-A1 优先权日:2013-03-04 标 题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) n n n n n n n n n n n n wherein n P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n R 1 is chlorodifluoromethyl or trifluoromethyl; n R 2 is optionally substituted aryl or optionally substituted heteroaryl; n n is 0 or 1; n including the process comprising n (a-i) reacting a compound of formula II n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; n with nitromethane in the presence a chiral catalyst to give a compound of formula III n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; and n (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. n n n n n The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:US-9233920-B2 优先权日:2010-06-11 标题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS; SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R 1 is chlorodifluoromethyl or trifluoromethyl; R 2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R 1 and R 2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R 1 and R 2 are as defined for the compound of formula I; and (a-ii) reductively cyclizing the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:US-9468207-B2 优先权日:2012-04-12 标 题 :Insecticide and acaricide paints that inhibit chitin synthesis, regulate insect juvenile hormone and repel arthropods, for controlling endemic diseases, pests and allergens 发明人:MATEO HERRERO MARIA PILAR 权利人:MATEO HERRERO MARIA PILAR 摘要:The present invention relates to insecticide and acaricide paints that inhibit chitin synthesis, regulate insect juvenile hormone and repel arthropods, for controlling endemic diseases, pests and allergens. The paints comprise at least the following compounds (in any combination): 1%-100% water, 0.0001%-20% insecticides, 0.0001%-20% chitin inhibitor, 0.0001%-20% juvenile hormone regulator, 1%-50% polymers, 0%-40% pigments, 0%-60% fillers, 0%-60% natural repellents, and 0.01%-20% stabilizers. The composition of the paints allows the active ingredients to be encapsulated in an aqueous polymer with or without the incorporation of fillers and pigments, and therefore the range of use thereof is increased.
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:US-2011230343-A1 优先权日:2008-10-24 标题 :Method for the Manufacture of Microparticles Comprising an Effect Substance 发明人:SCHROERS MICHAEL; DYLLICK-BRENZINGER RAINER; MERK MICHAEL; BARG HEIKO 权利人:BASF SE 摘要:A subject matter of the present invention is a process for the preparation of effect compound-comprising microparticles M comprising A) the formation of a crude suspension of microparticles A by means of enzymatic polyester synthesis in an inverse miniemulsion comprising enzyme, effect compound and polyester monomers; and B) the polymerization of wall monomers from the group consisting of ethylenically unsaturated monomers, polyisocyanates and polyepoxides in the crude suspension of microparticles A. Furthermore, the present invention relates to microparticles M which can be obtained by means of the process according to the invention and also to an agrochemical formulation comprising microparticles M. In addition, the present invention relates to the use of microparticles M prepared according to the invention as component in colorants, cosmetics, drugs, biocides, plant protection agents, fertilizers, additives for food or animal fodder, or auxiliaries for polymers, paper, textiles, leather, detergents or cleaners. Finally, the invention also relates to a method for combating undesirable plant growth, to a method for combating undesirable insect or acarid infestation on plants and/or for combating phytopathogenic fungi, and to seeds treated with the agrochemical formulation.
1: Mossa AT, Refaie AA, Ramadan A, Bouajila J. Antimutagenic effect of Origanum majorana L. essential oil against prallethrin-induced genotoxic damage in rat bone marrow cells. J Med Food. 2013 Dec;16(12):1101-7. doi: 10.1089/jmf.2013.0006. Epub 2013 Nov 6. doi: 10.1016/S1995-7645(14)60282-0. doi: 10.1155/2013/859085. Epub 2013 Dec 5. 4: Senthilkumaran S, Menezes RG, Balamurugan N, Thirumalaikolundusubramanian P. Prallethrin poisoning that taxes the brain. J Anaesthesiol Clin Pharmacol. 2014 Jan;30(1):116-7. doi: 10.4103/0970-9185.125726. 5: Chandra A, Dixit MB, Banavaliker JN. Prallethrin poisoning: A diagnostic dilemma. J Anaesthesiol Clin Pharmacol. 2013 Jan;29(1):121-2. doi: 10.4103/0970-9185.105820.
合成参考文献
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