CAS: 69308-37-8; (R)-4-Amino-3-(4-Chlorophenyl)Butanoic Acid

该化合物是一种化学化合物,被归类为肌肉放松剂,主要用于治疗与多发性硬化和脊髓损伤等条件有关的粘度,是伽马-氨丁酸(GABA)的衍生物,并且作为伽马-氨丁酸(GABA)的受体激动剂,有助于抑制过度...

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号290366-79-9 (R)-baclofen | CAS号63701-55-3 R-(+)-盐酸巴氯芬 | CAS号245662-60-6 1-[(3S)-3-(4-ch... | CAS号625457-56-9 (R)-ethyl 4-[(t... | CAS号20754-21-6 methyl 3-(4-chl... | CAS号104-88-1 对氯苯甲醛 | CAS号852051-18-4 methyl (R)-(+)-... | CAS号101671-01-6 p-chloro-beta-n...

合成工艺路线路线简述

    R(+)-巴氯芬盐酸盐置于sodium Hydroxide体系中,用 水 作为反应溶剂,以91%的收率获得产物(R)-巴氯芬
    参考文献:Method Of Producing Optically Active 4-Amino-3-Substituted Phenylbutanoic Acid
    标题:Method Of Producing Optically Active 4-Amino-3-Substituted Phenylbutanoic Acid
    摘要:本发明提供了生产化合物(iia)或化合物(iib)的方法,提供了生产化合物(iiia)或化合物(iiib)的方法,提供了生产化合物(va)或其盐或化合物(vb)或其盐的方法,提供了生产化合物(iiia)或化合物(iiib)的方法,此外,还提供了生产化合物(va)或其盐或化合物(vb)或其盐的方法,包括这些生产方法.

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:EP-3599246-A1
    优先权日:2018-07-25
    标题 :Means and methods for synthesizing precursors of y-aminobutyric acid (gaba) analogs
    发明人:POELARENDS GERRIT JAN; BIEWENGA LIEUWE; VAN DER MEER JAN-YTZEN; PODDAR HARSHWARDHAN; THANGAVELU SARAVANAN
    权利人:UNIV GRONINGEN
    摘要:The invention relates to the fields of drug development and biocatalysis, more specifically to a biocatalytic route for asymmetric synthesis of precursors of y-aminobutyric acid (GABA) analogs. Provided is an isolated mutant 4-oxalocrototonate tautomerase (4-OT) enzyme comprising the following mutations (i) leucine at position 8 substituted with a tyrosine (L8Y) or a phenylalanine (L8F); (ii) methionine at position 45 substituted with a tyrosine (M45Y); and (iii) phenylalanine at position 50 substituted with an alanine (F50A), wherein the positions are numbered according to the amino acid sequence of 4-OT ofPseudomonas putida.Also provided is a method for the synthesis of a precursor for the pharmaceutically relevant enantiomer of a GABA analog, comprising (i) providing a y-nitroaldehyde using the 4-OT mutant enzyme, followed by (ii) subjecting the thus obtained y-nitroaldehyde to an enzymatic oxidation reaction catalyzed by an aldehyde dehydrogenase (EC 1.2.1.3).

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:WO-9941229-A1
    优先权日:1998-02-11
    标题:Halogenated phenyl alcohol amides (ligands of gabab receptor) having an anticonvulsant activity
    发明人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE
    权利人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE
    摘要:New anticonvulsant compounds have been synthesized with a chlorine or fluorine atom in the position para of the phenyl ring. These compounds include DL-2-hydroxy-2-(4'-chlorophenyl)butyramide, DL-2-hydroxy-2-(4'-fluorophenyl)butyramide, DL-3-hydroxy-3-(4'-chlorophenyl)pentanamide, DL-3-hydroxy-3-(4'-fluorophenyl)pentanamide, DL-4-hydroxy-4-(4'-chlorophenyl)hexanamide and DL-4-hydroxy-4-(4'-fluorophenyl)hexanamide. Said compounds have a rather significant anticonvulsant activity against convulsions produced by pentylene tetrazol, as well as unexpected properties in particular a high affinity to the GABAB receptor in addition to a sustained anticonvulsant activity. The invention also relates to methods for the synthesis of halogenated phenyl alcohol amides such as indicated in the examples given in the disclosure.

    专利号:EP-2354120-A1
    优先权日:2003-08-20
    标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; YAO FENMEI; LUDWIKOW MARIA J; PHAN THU; PENG GE
    权利人:XENOPORT INC
    摘要:The present invention relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-tluorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The present invention also relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

    专利号:WO-2009094569-A2
    优先权日:2008-01-25
    标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
    宁波市海曙铭浩医药化工有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.mhpharm.com.cn
    企业联系电话:0574-88285925👤
    📞宁波市海曙铭浩医药化工有限公司 ⚠️参考联系方式
    联系人:盛先生 蔡小姐
    电话:0574-88285925
    手机:18657682767;13396618955
    传真:0574-88425889
    邮箱:sales@mhpharm.com.cn
    通信地址: 宁波市海曙区横街镇金泉路3号
    邮编: 317000
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    地址:宁波市海曙区横街镇金泉路3号
    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别
    ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    第 1 / 1 页

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Okuda DT, Kantor D, Jaros M, deVries T, Hunter S. Arbaclofen extended-release tablets for spasticity in multiple sclerosis: randomized, controlled clinical trial. Brain Commun. 2022 Nov 23;4(6):fcac300. doi: 10.1093/braincomms/fcac300.
    2: Aishworiya R, Valica T, Hagerman R, Restrepo B. An Update on Psychopharmacological Treatment of Autism Spectrum Disorder. Neurotherapeutics. 2022 Jan;19(1):248-262. doi: 10.1007/s13311-022-01183-1. Epub 2022 Jan 14.
    3: Frye RE. Clinical potential, safety, and tolerability of arbaclofen in the treatment of autism spectrum disorder. Drug Healthc Patient Saf. 2014 May 10;6:69-76. doi: 10.2147/DHPS.S39595.

    合成参考文献

    参考DOI号:10.1016/S0040-4020(96)00946-5
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知