4-叔丁基苄溴置于lithium Aluminium Tetrahydride,碘,Sodium Hydride,Magnesium体系中,用 四氢呋喃,乙醚 用作溶剂,化学反应 8.0H,反应生成喹螨醚 参考文献:Insecticidal Quinazoline Derivatives With (Trifluoromethyl)Diazirinyl And Azido Substituents As Nadh:Ubiquinone Oxidoreductase Inhibitors And Candidate Photoaffinity Probes 标题:Insecticidal Quinazoline Derivatives With (Trifluoromethyl)Diazirinyl And Azido Substituents As Nadh:Ubiquinone Oxidoreductase Inhibitors And Candidate Photoaffinity Probes 摘要:Two Candidate Photoaffinity Probes Are Designed From 4-Substituted Quinazolines Known To Be Potent Insecticides/acaricides And Nadh:Ubiquinone Oxidoreductase Inhibitors Acting At Or Near The Rotenone Site. 4-(11-Azidoundecyl-2-Amino)Quinazoline,Based On The Undecylamino Analog San 548A As A Prototype,Was Synthesized In 18% Overall Yield From Ethyl 10-Undecenoate By Oxidation Of The Terminal Double Bond,Reductive Amination,Coupling To 4-Chloroquinazoline,And Functional Group Manipulation Of The Terminal Ethyl Ester To An Alcohol,A Mesylate And Finally Nucleophilic Displacement With Azide Ions. 4-(4-(3-(Trifluoromethyl)3H-Diazirin-3-yl)Phenethoxy)Quinazoline [the (Trifluoromethyl)Diazirinyl Analog Of Fenazaquin Insecticide/acaricide] Was Prepared From 4-Bromophenethyl Alcohol In 31% Overall Yield By First Introducing The Trifluoromethylketone Moiety Followed By Its Conversion To The (Trifluoromethyl)Diazirine And Finally Coupling To 8-Chloroquinazoline As Above. Both Candidate Photoaffinity Probes Have The Inhibitory Potency Of Rotenone (Ic50 Of 3-4 Nm In Each Case). The Azidoundecylamino Compound Has Inadequate Photoreactivity Whereas That Of The (Trifluoromethyl)Diazirinyl Analog Is Ideal At 350 Nm. Radiosynthesis Of The Latter Photoaffinity Ligand Included Introduction Of The Diazirinyl Moiety As The Carbene Precursor,Oxidation Of (Trifluoromethyl)Diazirinylphenethyl Alcohol To The Corresponding Acid With Jones' Reagent,And Reduction Of The Phenacetyl Chloride Intermediate With Sodium Borotritide To Incorporate Tritium. Doi:10.1021/tx9501602
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:US-9919064-B2 优先权日:2012-08-10 标 题 :Compositions, methods, and systems for the synthesis and use of imaging agents 发明人:CESATI RICHARD R; RADEKE HEIKE S; PANDEY SURESH K; PUROHIT AJAY; ROBINSON SIMON P 权利人:LANTHEUS MEDICAL IMAGING INC 摘要:The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
专利号:US-2007232495-A1 优先权日:2006-03-24 标题:Compositions and methods to add value to plant products, increasing the commercial quality, resistance to external factors and polyphenol content thereof 发明人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 权利人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 摘要:The invention is related to compositions and methods that naturally protect plant tissues against ultraviolet radiation and temperature, thus giving protection against sunburn to plants, plant parts, fruits and/or flowers during their development. The invention is also related to compositions and methods to naturally improve the color of plants, plant parts, fruits and/or flowers by inducing the natural synthesis of flavonoids and anthocyanins present in plants. Likewise, the present invention is directed to improving the nutritional value of plants, plant parts, fruits and/or flowers by increasing the normal levels of polyphenolic compounds, especially flavonoids, present therein. Additionally, the present invention is related to compositions and methods that give more resistance to plants, plant parts, fruits and/or flowers against pathogens as bacteria and fungi. Finally, the present invention is related to plants, plant parts, fruits, flowers and/or propagating material treated with the compositions described in the present document.
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.
1: DeGroot DE, Swank A, Thomas RS, Strynar M, Lee MY, Carmichael PL, Simmons SO. mRNA transfection retrofits cell-based assays with xenobiotic metabolism. J Pharmacol Toxicol Methods. 2018 Mar 16;92:77-94. doi: 10.1016/j.vascn.2018.03.002. [Epub ahead of print] doi: 10.1016/j.chroma.2017.11.048. Epub 2017 Nov 22. doi: 10.1007/s11011-017-0137-7. Epub 2017 Oct 27. doi: 10.1603/EC14234. doi: 10.1007/s10493-014-9830-y. Epub 2014 Jun 30. Available from http://www.ncbi.nlm.nih.gov/books/NBK83579/ doi: 10.1007/s00128-011-0318-8. Epub 2011 Jun 12. doi: 10.1111/j.1471-4159.2011.07175.x. Epub 2011 Jan 28. 10: Fanigliulo A, Massa CG, Ielpo L, Pacella R, Crescenzi A. Evaluation of the efficacy of Oberon (Spiromesifen), to contain infestations of mites and whiteflies on Capsicum annuum L. Commun Agric Appl Biol Sci. 2010;75(3):341-4. doi: 10.1016/j.chroma.2009.10.040. Epub 2009 Oct 28. doi: 10.1007/s00128-009-9863-9. Epub 2009 Oct 22. doi: 10.1007/s00216-009-3133-x. Epub 2009 Sep 25. doi: 10.1016/j.chroma.2009.08.012. Epub 2009 Aug 13. doi: 10.1080/02652030902896194. doi: 10.1080/02652030902839731. doi: 10.1016/j.chroma.2008.08.059. Epub 2008 Aug 20. doi: 10.1017/S0007485308006081. Epub 2008 Jul 1.
合成参考文献
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