CAS: 36531-26-7; (E)-3-(2-(1-Methyl-1,4,5,6-Tetrahydropyrimidin-2-yl)Vinyl)Phenol

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    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:WO-2021009026-A1
    优先权日:2019-07-12
    标 题 :Methyl 2-[(4-methoxyimino-tetralin-6-yl]prop-2-enoate derivatives, chromane, isochromane, 6,7,8,9-tetrahydrobenzo[7]annulene, 1h-isobenzofurane and indane analogues thereof, and similar compounds, as agrochemical fungicides
    发明人:WEISS MATTHIAS; WILLIAMS SIMON; RENDINE STEFANO; BOU HAMDAN FARHAN; HOFFMAN THOMAS; QUARANTA LAURA
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:Compounds of formula (I): (Formula (I)) Formula (I) encompasses e.g. tetraline, chromane, isochromane, 6,7,8,9-tetrahydrobenzo[7]annulene, 1H-isobenzofurane and indane derivatives. The compounds of formula (I) are useful as a pesticides, especially as fungicides. The present description discloses the synthesis and characterisation of exemplary compounds as well as biological data thereof (e.g. pages 53 to 78; examples 1 to 10; table T1; compounds 1.1 to 1.54; examples A and B). Preferred compounds are e.g.: Methyl (E)-3-methoxy-2-[(4E)-4-methoxyimino-7-methyl-tetralin-6- yl]prop-2-enoate (example 2; compound 1.6 of table T1): (Formula (A)). Methyl (E)-3-methoxy-2-[(4Z)-4-methoxyiminoisochroman-6-yl]prop-2- enoate (example 6; compound 1.39 of table T1): (Formula (B))

    专利号:US-2008176865-A1
    优先权日:2005-06-15
    标 题:Substituted arylpyrazoles
    发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
    权利人:PFIZER LTD
    摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

    专利号:US-7645786-B2
    优先权日:2005-06-15
    标题:Substituted arylpyrazoles
    发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
    权利人:PFIZER
    摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

    专利号:US-7803832-B2
    优先权日:2004-03-18
    标题 :N-(1-arylpyrazol-4L)sulfonamides and their use as parasiticides
    发明人:CRITCHER DOUGLAS JAMES; WALSHE NIGEL DEREK ARTHUR; LAURET CHRISTELLE
    权利人:PFIZER; PFIZER PROD INC
    摘要:The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R 1 -R 5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
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    主要参考文献


    1: Pfarr KM, Krome AK, Al-Obaidi I, Batchelor H, Vaillant M, Hoerauf A, Opoku NO, Kuesel AC. The pipeline for drugs for control and elimination of neglected tropical diseases: 2. Oral anti-infective drugs and drug combinations for off- label use. Parasit Vectors. 2023 Oct 31;16(1):394. doi: 10.1186/s13071-023-05909-8.
    2: Schärer A, Biendl S, Keiser J. Trichuris muris egg-hatching assay for anthelminthic drug discovery and characterization. Int J Parasitol Drugs Drug Resist. 2023 Dec;23:63-70. doi: 10.1016/j.ijpddr.2023.10.001. Epub 2023 Oct 9.
    3: Easland E, Biendl S, Keiser J. Development of a hookworm egg hatching assay to determine the ovicidal effects of anthelminthics. Parasit Vectors. 2023 May 4;16(1):157. doi: 10.1186/s13071-023-05771-8.

    合成参考文献


    参考文献:10.1007/s00436-001-0535-x
    摘要:Harder A. Chemotherapeutic approaches to nematodes: current knowledge and outlook. Parasitol Res. 2002 Mar;88(3):272–7. doi: 10.1007/s00436-001-0535-x.
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