CAS: 85068-29-7; (3,5-Bis(Trifluoromethyl)Phenyl)Methanamine

该化合物是一种氟芳烃,其特点是在苯基环的3和5个位置上存在两个三氟甲基组,这种结构特征具有高电子提取特性,在核生殖替代和凝聚反应中增强了其反应性.该化合物被广泛用作制药和农用化学合成的关键中间体,特别是在开发需要强化代谢稳定性和亲脂性的积极成分方面.其三氟甲基组有助于改善生物利用率和抗酶降解.苯基胺会进一步促进功能化,使其成为精细化学应用的多用途建筑块.由于对湿度和空气的敏感性,适合在惰性条件下使用.

结构式图片

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

上下游产品

CAS号401-95-6 3,5-双(三氟甲基)苯甲醛 | CAS号511256-30-7 N-benzyl-1-(3,5... | CAS号27126-93-8 3,5-双(三氟甲基)苯甲腈 | CAS号676557-17-8 N-[3,5-Bis(trif...

合成工艺路线路线简述

  • 27126-93-8 = 85068-29-7
    反应条件:1.1 Reagents: Hydrogen,Ammonia Catalysts: Nickel Solvents: Methanol; 18 H,35 Bar,60 °C
    标题:Stable And Reusable Ni-Based Nanoparticles For General And Selective Hydrogenation Of Nitriles To Amines
    作者:Ma,Zhuang; Chandrashekhar,Vishwas G.; Zhou,Bei; Alenad,Asma M.; Rockstroh,Nils; Et Al
    参考文献:Chemical Science 日期:2022 卷标:13(36) 页码:10914-10922]

    27126-93-8 = 85068-29-7
    反应条件:1.1 Reagents: Hydrogen,Ammonia Catalysts: Iron Oxide (Fe2O3),Iron Solvents: Isopropanol; 24 H,50 Bar,120 °C
    标题:Silica-Supported Fe/fe-O Nanoparticles For The Catalytic Hydrogenation Of Nitriles To Amines In The Presence Of Aluminium Additives
    作者:Chandrashekhar,Vishwas G.; Senthamarai,Thirusangumurugan; Kadam,Ravishankar G.; Malina,Ondrej; Kaslik,Josef; Et Al
    参考文献:Nature Catalysis 日期:2022 卷标:5(1) 页码:20-29]

    27126-93-8 = 85068-29-7
    反应条件:1.1 Reagents: Oxalic Acid Catalysts: Iron Oxide (Fe3O4),Palladium,Titania; 2 H,Rt
    标题:Preparation Of A Magnetic Mesoporous Fe3O4-Pd@tio2 Photocatalyst For The Efficient Selective Reduction Of Aromatic Cyanides
    作者:Zhao,Ziming; Long,Yu; Luo,Sha; Wu,Wei; Ma,Jiantai
    参考文献:New Journal Of Chemistry 日期:2019 卷标:43(16) 页码:6294-6302]

    848825-79-6 = 85068-29-7
    反应条件:1.1 Reagents: Hydrogen,Ammonium Hydroxide Catalysts: Nickel Solvents: Isopropanol; 6 - 8 H,70 - 80 Psi,25 - 35 °C
    标题:Asymmetric Organocatalysis And Continuous Chemistry For An Efficient And Cost-Competitive Process To Pregabalin
    作者:Carlone,Armando; Bernardi,Luca; Mccormack,Peter; Warr,Tony; Oruganti,Srinivas; Et Al
    参考文献:Organic Process Research & Development 日期:2021 卷标:25(12) 页码:2795-2805]

    401-95-6 = 85068-29-7
    反应条件:1.1 Reagents: 1,8-Diazabicyclo[5.4.0]Undec-7-Ene,Sulfuric Acid Magnesium Salt (1:1),Benzeneacetic Acid,α-Amino-α-Methyl-,Potassium Salt (1:1) Solvents: 1,4-Dioxane; 24 H,50 °C1.2 Reagents: Hydroxylamine Solvents: Water; 15 Min,Rt
    标题:Transamination Of Aromatic Aldehydes To Primary Arylmethylamines
    作者:Cai,Weiqi; Yang,Yue; Ma,Jiguo; Cao,Jing; Ren,Xinyi; Et Al
    参考文献:Organic Letters 日期:2023 卷标:25(21) 页码:3876-3880
3,5-双三氟甲基苯甲醛置于magnesium Sulfate,1,8-二氮杂双环[5.4.0]十一碳-7-烯,Potassium 2-Amino-2-Phenylpropanoate体系中,用 1,4-二氧六环 作为反应溶剂,以54 %的收率获得产物3,5-双(三氟甲基)苄胺
参考文献:芳香醛与伯芳基甲胺的转氨作用
标题:芳香醛与伯芳基甲胺的转氨作用
摘要:在 2-氨基-2-苯基丙酸盐(2A或2E)作为胺源存在的情况下,芳香醛在非常温和的条件下进行脱羧氨基转移,以 44-99% 的收率生产各种芳基甲胺.该工作为伯芳基甲胺的合成提供了一种高效的新方法.
DOI:10.1021/acs.Orglett.3C01234

海关参考信息

专利信息


专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-2025049791-A1
优先权日:2023-08-03
标题:Synthesis of MEK7 Inhibitors and methods of Use Thereof
发明人:SCHEIDT KARL A; KIM DALTON ROBERT; ORR MEGHAN JO
权利人:UNIV NORTHWESTERN
摘要:Disclosed herein are 4-phenoxypyrimidine compounds and derivatives thereof for use as inhibitors of mitogen-activated protein kinase 7 (MEK7). The disclosed compounds and pharmaceutical compositions thereof may be used in methods for treating a disease or disorder associated with MEK7 activity, including cell proliferative diseases and disorders associated with MEK7 activity, such as cancer.

专利号:EP-0789577-A1
优先权日:1995-06-07
标 题:Synthesis of n-substituted oligomers

专利号:EP-0789577-B1
优先权日:1995-06-07
标 题:Synthesis of n-substituted oligomers

专利号:WO-9931506-A1
优先权日:1997-12-18
标题 :Parallel solution phase synthesis of lactams

专利号:WO-9640202-A1
优先权日:1995-06-07
标 题:Synthesis of n-substituted oligomers
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主要参考文献

[参考文献]: Lihu Yang, Et Al. Discovery Of 3,5-Bis(Trifluoromethyl)Benzyl L-Arylglycinamide Based Potent Ccr2 Antagonists. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3735-9.

合成参考文献


参考文献:10.1055/s-0040-1706919
摘要:Point to Mechanically Chiral Planes. Synfacts. 2020 Jul 21;16(08):0917. doi: 10.1055/s-0040-1706919.
参考文献:10.1055/s-0034-1380382
摘要:Miura T, Nakashima K, Kawada M, Hirashima S, Kato M, Koseki Y. Asymmetric Conjugate Addition of Ketones to Maleimides Using Diaminomethyleneindenedione Organocatalyst. Synlett. 2015 Mar 19;26(09):1248–52. doi: 10.1055/s-0034-1380382.
参考文献:10.1134/s0036024422130179
摘要:Sivasankari K, Karthikeyan B. Self-Assembled Nanotubes of Benzyl Derivative Phenylalanine and a New Method for Water Purification: An Initiative towards Sustainable Affordable Safe Water. Russ. J. Phys. Chem. 2022 Dec;96(13):2948–52. doi: 10.1134/s0036024422130179.
参考文献:10.1038/s43246-024-00623-z
摘要:Jirát-Ziółkowska N, Sulková K, Kracíková L, Androvič L, Havliček D, Laga R, Jirák D. Bio-responsive polymers for dual 31P/19F-magnetic resonance to detect reactive oxygen species in vivo. Commun Mater. 2024 Sep 05;5(1). doi: 10.1038/s43246-024-00623-z.
参考文献:10.1631/bdm.2500054
摘要:Gao Y, Zhang M, Chen Q, Lin Y, Wu C, Pan X, Guo L, Hiew TN, Huang Z. Polymeric micelles: “magic bullets” for cancer treatment. Bio-des. Manuf. 2025 Nov;8(6):1103–25. doi: 10.1631/bdm.2500054.
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