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-4337274-A 优先权日:1978-05-30 标 题 :Flukicidal compounds 发明人:GORVIN JOHN H 权利人:BURROUGHS WELLCOME CO 摘要:Diphenylethers of the formula: ##STR1## their synthesis, formulations containing them, methods of making such formulations, and their use in the treatment of liver fluke infections in mammals.
1: Kotze AC, Ruffell AP, Ingham AB. Phenobarbital induction and chemical synergism demonstrate the role of UDP-glucuronosyltransferases in detoxification of naphthalophos by Haemonchus contortus larvae. Antimicrob Agents Chemother. 2014 Dec;58(12):7475-83. doi: 10.1128/AAC.03333-14. Epub 2014 Oct 6. 2: Fiel C, Guzmán M, Steffan P, Rodriguez E, Prieto O, Bhushan C. The efficacy of trichlorphon and naphthalophos against multiple anthelmintic-resistant nematodes of naturally infected sheep in Argentina. Parasitol Res. 2011 Aug;109 Suppl 1:S139-48. doi: 10.1007/s00436-011-2410-8.
合成参考文献
摘要:World Review of Pest Control., 9(119), 1970 摘要:Schafer, E.W. 1972. The acute oral toxicity of 369 pesticidal, pharmaceutical and other chemicals to wild birds. Toxicology and Applied Pharmacology. 21:315-330. 摘要:Schafer, E. W., Jr., W. A. Bowles Jr., and J. Hurlbut. 1983. The acute oral toxicity and repellency and hazard potential of 998 chemicals to one or more species of wild and domestic birds. Archives of Environmental Contamination and Toxicology 12:355-382. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 2004. Toxicity, Repellency of Phytotoxicity of 979 Chemicals to Birds, Mammals and Plants. Research Report No. 04-01. National Wildlife Research Center, Fort Collins, Colorado. 118 pp. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/U_schafer041_2004.pdf