N-甲基-N'-(2,4-二甲基苯基)硫脲,氯乙醛缩二乙醇,Hydroxide置于乙醚,水,Sodium Sulfate-Iii体系中,用 盐酸 作为反应溶剂,化学反应 1.0H,反应生成 N-3-甲基-4-亚噻唑-2-基-2,4-二甲基苯胺 参考文献:Phenylimino-Thiazolines And Their Use As Acaricides 标题:Phenylimino-Thiazolines And Their Use As Acaricides 摘要:这是一段关于杀螨化合物的描述,其通用公式为##str1##其中r.Sub.1和r.Sub.2分别独立地表示氯,甲基或乙基,其中r.Sub.2可以占据4-或6-位置,但如果r.Sub.1和r.Sub.2表示氯,则r.Sub.2不能在4-位置,R.Sub.3表示具有1至4个碳原子的直链或支链烷基,可选地被1-2个碳原子的烷氧基取代,或具有3至5个碳原子的直链或支链烯基,可选地被卤素取代,包括酸加成盐,特别是盐酸盐,以及含有这些化合物的组合物,以及使用这些化合物对抗螨虫,特别是蜱虫.
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: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-6921770-B2 优先权日:2000-07-28 标题:2-Phenyliminothiazolines, their preparation method and anti-rice blast agent containing the same 发明人:HAHN HOH GYU; NAM KEE DAL; CHANG KEE HYUK; CHO KWANG YUN; KIM HEUNG TAE 权利人:KOREA INST SCI & TECH 摘要:2-phenyliminothiazolines of the following formula I, their salts, their preparation method and their use for treating rice blast. The phenyliminothiazolines and their salts of the present invention have low toxicity to environment or living organisms, and exert high activity at low concentration for treating rice blast through a new control mechanism, that is by inhibiting pentaketide synthesis and cyclization of the melanin sythesis process in formula I
1: Zheng W, Park JA, Abd El-Aty AM, Kim SK, Cho SH, Choi JM, Yi H, Cho SM, Ramadan A, Jeong JH, Shim JH, Shin HC. Development and validation of modified QuEChERS method coupled with LC-MS/MS for simultaneous determination of cymiazole, fipronil, coumaphos, fluvalinate, amitraz, and its metabolite in various types of honey and royal jelly. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Jan 1;1072:60-69. doi: 10.1016/j.jchromb.2017.11.011. Epub 2017 Nov 8. doi: 10.1002/ps.4161. Epub 2015 Oct 27. Epub 2005 Nov 23.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1016/j.mrgentox.2005.10.003 摘要:Stanimirovic Z, Stevanovic J, Jovanovic S, Andjelkovic M. Evaluation of genotoxic effects of Apitol® (cymiazole hydrochloride) in vitro by measurement of sister chromatid exchange. Mutation Research/Genetic Toxicology and Environmental Mutagenesis. 2005 Dec;588(2):152–7. doi: 10.1016/j.mrgentox.2005.10.003.