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:EP-1306084-B1 优先权日:1998-06-09 标 题 :Compositions for the control of parasitic infestations in fish 发明人:ALEXANDER SVEIN; EVENSEN OYSTEIN; SYVERTSEN CHRISTIAN; MARTINSEN BERNT 权利人:PHARMAQ AS 摘要:Injectable compositions comprising antiparasitically active chitin synthesis inhibitor substances are described, for controlling parasitic infestations including infestations with sea lice and isopod species in farmed fish. The compositions are optionally formulated in a fish vaccine. The antiparasitically active chitin synthesis inhibitor substances protect the fish against parasites for a substantial period of time after injection. Useful embodiments include compositions with lufenuron that confer protection against new parasitic infestation for an extended period of time after treatment.
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.
专利号:US-11213031-B2 优先权日:2017-11-13 标 题:Tetrazolylpropyl derivatives and their use as fungicides 发明人:SUDAU ALEXANDER; HOFFMANN SEBASTIAN; DAHMEN PETER; WEBSTER ROBERT ALAN; MEISSNER RUTH; GOERTZ ANDREAS; MILLER RICARDA; COQUERON PIERRE-YVES; BERNIER DAVID; NICOLAS LIONEL; BRUNET STEPHANE; KENNEL PHILIPPE; TOQUIN VALERIE; GOURGUES MATHIEU; LOQUE DOMINIQUE; THOMAS VINCENT 权利人:BAYER AG; BAYER CROPSCIENCE AG 摘要:The present invention relates to tetrazolylpropyl derivatives of formula (I) n nwherein one of V 1 and V 2 represents CR 3 and the other one of V 1 and V 2 represents N, Q represents a 6-membered aromatic cycle as defined in the specification, and R 1 , R 2 , R 3 , R 4 , and R 5 are defined as disclosed in the specification, to compositions comprising such compounds, to the use of said compounds as fungicides, as well as to particular intermediates useful in the synthesis of said tetrazolylpropyl derivatives.
1: Kaur K, Helgesen KO, Bakke MJ, Horsberg TE. Mechanism behind Resistance against the Organophosphate Azamethiphos in Salmon Lice (Lepeophtheirus salmonis). PLoS One. 2015 Apr 20;10(4):e0124220. doi: 10.1371/journal.pone.0124220. eCollection 2015. 2: Olsvik PA, Ørnsrud R, Lunestad BT, Steine N, Fredriksen BN. Transcriptional responses in Atlantic salmon (Salmo salar) exposed to deltamethrin, alone or in combination with azamethiphos. Comp Biochem Physiol C Toxicol Pharmacol. 2014 May;162:23-33. doi: 10.1016/j.cbpc.2014.03.005. Epub 2014 Mar 24. doi: 10.1016/j.ecoenv.2014.11.016. Epub 2014 Dec 9. doi: 10.1016/j.prevetmed.2015.09.017. Epub 2015 Oct 9. doi: 10.1016/j.ecoenv.2016.08.019. Epub 2016 Sep 2. doi: 10.1371/journal.pone.0149264. eCollection 2016. 7: Canty MN, Hagger JA, Moore RT, Cooper L, Galloway TS. Sublethal impact of short term exposure to the organophosphate pesticide azamethiphos in the marine mollusc Mytilus edulis. Mar Pollut Bull. 2007 Apr;54(4):396-402. Epub 2007 Jan 30. pii: E304. doi: 10.3390/ijms17050304.
合成参考文献
参考文献:10.1007/s00244-014-0038-2 摘要:Pinto MI, Micaelo C, Vale C, Sontag G, Noronha JP. Screening of Priority Pesticides in Ulva sp. Seaweeds by Selective Pressurized Solvent Extraction Before Gas Chromatography with Electron Capture Detector Analysis. Archives of Environmental Contamination and Toxicology. 2014 May 23;67(4):547–56. doi: 10.1007/s00244-014-0038-2. 参考文献:10.1016/j.cbpb.2006.07.005 摘要:Romani R, Corsi I, Bonacci S, Focardi S, De Medio GE, De Santis A, Incarnato F, Giovannini E, Rosi G. Organophosphate-resistant forms of acetylcholinesterases in two scallops—the Antarctic Adamussium colbecki and the Mediterranean Pecten jacobaeus. Comparative Biochemistry and Physiology Part B: Biochemistry and Molecular Biology. 2006 Oct;145(2):188–96. doi: 10.1016/j.cbpb.2006.07.005.