📜2,4-二氯-6-甲基嘧啶,二甲胺置于silica Gel,乙酸乙酯,甲醇,Hexanes体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.5H,以to Give 2-Chloro-4-Dimethylamino-6-Methylpyrimidine (4.18 G,40%) As A Pale Yellow Solid的收率获得产物鼠立死 参考文献:Novel Quinoline,Tetrahydroquinazoline,And Pyrimidine Derivatives And Methods Of Treatment Related To The Use Thereof 标题:Novel Quinoline,Tetrahydroquinazoline,And Pyrimidine Derivatives And Methods Of Treatment Related To The Use Thereof 摘要:本发明涉及一种新的化合物,其化学式为(I),该化合物作为mch受体拮抗剂.这些组合物在制药组合物中的应用包括预防或治疗改善记忆功能,睡眠和觉醒,焦虑,抑郁,情绪障碍,癫痫,肥胖症,糖尿病,食欲和进食障碍,心血管疾病,高血压,血脂异常,心肌梗死,暴食症包括贪食症,厌食症,精神障碍包括躁郁症,精神分裂症,谵妄,痴呆,压力,认知障碍,注意力缺陷障碍,物质滥用障碍和运动障碍包括帕金森病,癫痫和成瘾等.
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))
摘要:Wirksubstanzen der Pflanzenschutz und Schadlingsbekampfungsmittel, Perkow, W., Berlin, Verlag Paul Parey, 1971-1976, -(-), 1971/1976 摘要:Journal of the American Pharmaceutical Association, Scientific Edition., 37(307), 1948 摘要:Agrochemicals Handbook, with updates, Hartley, D., and H. Kidd, eds., Nottingham, Royal Soc of Chemistry, 1983-86, A099(1983) 摘要:Pesticide Index, Frear, E.H., ed., State College, PA, College Science Pub., 1969, 5(59), 1976 摘要:40 CFR 355; U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of June 21, 2006: https://www.ecfr.gov