CAS: 459-31-4; 3-(4-Fluorophenyl)Propanoic Acid

该化合物是一种含分子式C9H9FO2的氟芳芳烃式的盒式盒式酸,该化合物是有机合成的多用途中间体,特别是在制药和农用化学应用方面;氟替代物的存在增强了其反应性和稳定性,使其对构建更复杂的分子很有价值;其箱式酸功能允许进一步衍生,如酯化或恐吓;复合物具有一贯的纯度,具有可靠的物理化学特性,确保研究和工业过程的再生性;它通常用于开发活性药物成分和精细化学品.

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CAS号459-32-5 对氟肉桂酸 | CAS号3984-22-3 2-乙烯基-1,3-二氧戊环 | CAS号460-00-4 对氟溴苯 | CAS号7116-38-3 3-(4-氟苯基)丙酸乙酯 | CAS号459-46-1 对氟溴苄 | CAS号105-53-3 丙二酸二乙酯 | CAS号1765-93-1 4-氟苯硼酸 | CAS号79-10-7 丙烯酸 | CAS号7589-27-7 对氟苯乙醇 | CAS号405-50-5 对氟苯乙酸 | CAS号24484-55-7 1-(3-溴丙基)-4-氟苯 | CAS号2928-14-5 3-(4-氟苯基)丙酸甲酯 | CAS号63416-70-6 3-(4-氟苯基)丙醛 | CAS号1481-32-9 6-氟-1-茚酮 | CAS号702-15-8 4-氟苯丙醇 | CAS号52031-15-9 5-氟-1H-茚 | CAS号52085-94-6 6-氟-2,3-二氢-茚-1-醇

合成工艺路线路线简述

    对氟肉桂酸置于palladium Diacetate,频那醇硼烷体系中,用 二氯甲烷 作为反应溶剂,化学反应 12.0H,以99%的收率获得产物3-(4-氟苯基)丙酸
    参考文献:广义化学选择性转移加氢/氢化氘
    标题:广义化学选择性转移加氢/氢化氘
    摘要:使用hbpin和各种质子试剂作为氢源,已经开发了一种普遍,简单而有效的不饱和键转移加氢方法.包括烯烃,炔烃,芳族杂环,醛,酮,亚胺,偶氮,硝基,环氧和腈化合物在内的所有底物均应用于该催化体系.可以容忍在pd / C / H 2组合下无法生存的各种基团.研究了反应物的活性,其变化趋势为:苯乙烯>二苯基甲亚胺>苯甲醛>偶氮苯>硝基苯>喹啉>苯乙酮>苄腈.还研究了带有两个或多个不同不饱和键的底物,并以优异的化学选择性发生了转移氢化.由pd(oac)2和hbpin反应生成的二氧化钛极大地提高了th效率.此外,使用d 2 O和hbpin通过原位hd反应生成和区分,实现了末端芳族烯烃的化学选择性抗markovnikov加氢氘.
    DOI:10.1002/adsc.202000759

    海关参考信息

    专利信息


    专利号:US-2003092064-A1
    优先权日:2001-04-05
    标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof
    发明人:READER JOHN C
    权利人:MILLENNIUM PHARM INC
    摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.

    专利号:WO-2015131100-A1
    优先权日:2014-02-28
    标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
    发明人:YU JIN-QUAN
    权利人:SCRIPPS RESEARCH INST
    摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

    专利号:US-5175294-A
    优先权日:1989-11-24
    标 题:New thiophene compounds as intermediates
    发明人:WIERZBICKI MICHEL; SAUVEUR FREDERIC; BONNET JACQUELINE; BRISSET MARTINE; TORDJMAN CHARLES
    权利人:ADIR
    摘要:New thiophene compounds of the formula: in which: X represents hydrogen, halogen, C1-C5alkyl or alkoxy or dialkylamino; n represents 1 or 2; a represents an integer of from 2 to 6; b represents 2 or 3; c represents 1 or 2, and is such that b+c=4; R1 and R2 represent hydrogen or (C1-C5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; and R and R' represent hydrogen or (C1-C5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts. The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue. As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: in which: X, n, a, b, c, R1, R2, R and R' are as above defined.

    专利号:US-12304894-B2
    优先权日:2019-04-17
    标题 :Derivatives of adamantyl oxadiazoles and pharmaceutically acceptable solvates, hydrates and salts thereof, pharmaceutical composition comprising same, synthesis method, suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1)
    发明人:FARDELLA BELLO CARLOS ENRIQUE; LAGOS ARÉVALO CARLOS FERNANDO; VECCHIOLA CÃ?RDENAS ANDREA PAOLA; ALLENDE SANZANA FIDEL ALEJANDRO; DIETHELM VARELA BENJAMIN MANUEL; RECABARREN GAJARDO GONZALO IVAN; GONZÃ?LEZ CISTERNA PABLO MARCELO
    权利人:UNIV PONTIFICIA CATOLICA CHILE
    摘要:The present invention relates to compounds derived from adamantyl oxadiazoles and the pharmaceutically acceptable solvates, hydrates and salts of same. These compounds are suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1), as well as in the production of a drug for treating conditions and diseases such as high blood pressure, obesity, dyslipidaemia, type 2 diabetes, insulin resistance, glaucoma, metabolic syndrome, cognitive disorders, osteoporosis, immune disorders, depression and other conditions. Also provided is a pharmaceutical composition comprising the compounds and a method for preparing said composition.

    专利号:US-5061704-A
    优先权日:1989-11-24
    标题:Thiophene compounds, compositions and use
    发明人:WIERZBICKI MICHEL; SAUVEUR FREDERIC; BONNET JACQUELINE; BRISSET MARTINE; TORDJMAN CHARLES
    权利人:ADIR
    摘要:1. New thiophene compounds of the formula: in which: X represents hydrogen, halogen, C1-C5alkyl or alkoxy or dialkylamino; n represents 1 or 2; a represents an integer of from 2 to 6; b represents 2 or 3; c represents 1 or 2, and is such that b+c=4; R1 and R2 represent hydrogen or (C1-C5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; and R and R' represent hydrogen or (C1-C5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts. The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue. 2. As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: in which: X, n, a, b, c, R1, R2, R and R' are as above defined.

    专利号:US-10308595-B2
    优先权日:2013-02-15
    标 题:Albicidin derivatives, their use and synthesis
    发明人:SUESSMUTH RODERICH; KRETZ JULIAN; SCHUBERT VIVIEN; PESIC ALEXANDER; HUEGELLAND MANUELA; ROYER MONIQUE; COCIANCICH STEPHANE; ROTT PHILIPPE; KERWAT DENNIS; GRAETZ STEFAN
    权利人:UNIV BERLIN TECH
    摘要:Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.
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    合成参考文献


    摘要:Merino, P., Science of Synthesis, (2010) 45, 289.
    摘要:Clarke, M. L.; Fuentes, J. A., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 248.
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