CAS: 88050-17-3; Fmoc-Hyp-Oh

该化合物是氨酸分泌物的一种衍生物,专门用氟基甲基氧碳基(Fmoc)保护团在氮原子上进行修改,其特点是,由于Fmoc组在基本条件下的稳定性和在温和酸条件下易于去除,它能够成为peptide合成的一块构件,特别是固相合成(SPS),因此,这种合成物具有作为peptide合成的构件,特别是固相聚(SPS)的构件的能力,因为Fmoc组在基本条件下稳定,在温和酸条件下易于去除. 4-Hydroxproline的4-Hydroxproline组在Proline Protephids的成份和稳定性方面具有独特的特性,可以影响peptides的相容合和稳定性.Fmoc-L-4-Hydroxproline在Pep化学领域是一种宝贵的化合物.

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号51-35-4 L-羟脯氨酸 | CAS号82911-69-1 9-芴甲基-N-琥珀酰亚胺碳酸酯 | CAS号7536-89-2 trimethylsilyl ... | CAS号122350-59-8 (4R)-N-Fm°C-4-羟... | CAS号748165-40-4 (2s,4s)-4-氟吡咯烷-2-羧酰胺

合成工艺路线路线简述

  • 合成目标产物 Fmoc-L-Hydroxyproline 主要起始原料 9-Fluorenylmethyl Chloroformate And L-Hydroxyproline
  • 51-35-4 + 82911-69-1 = 88050-17-3
    反应条件:1.1 Reagents: N-Methyl-N-(Trimethylsilyl)Trifluoroacetamide Solvents: Dichloromethane1.2 Solvents: Dichloromethane1.3 Reagents: Methanol
    标题:An Efficient Procedure For The Preparation Of Fmoc-Amino Acids
    作者:Raillard,Stephen P.; Et Al
    参考文献:Organic Preparations And Procedures International 日期:1998 卷标:30(2) 页码:183-186
Trimethylsilyl (2S,4R)-4-(Trimethylsilyoxy)Pyrrolidine-2-Carboxylate置于甲醇体系中,用 二氯甲烷 作为反应溶剂,化学反应 4.0H,反应生成 Fmoc-L-4-羟基脯氨酸
参考文献:An Efficient Procedure For The Preparation Of Fmoc-Amino Acids
标题:An Efficient Procedure For The Preparation Of Fmoc-Amino Acids
摘要:
DOI:10.1080/00304949809355277

海关参考信息

专利信息


专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人:DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-8569452-B2
优先权日:2011-02-17
标题:Preparation of phalloidin and its derivatives
发明人:LIU BAOSHENG; ZHANG JIANHENG
权利人:LIU BAOSHENG; ZHANG JIANHENG; AMERICAN PEPTIDE COMPANY INC
摘要:The present invention relates to novel phalloidin derivatives and their fluorescent dye conjugates. These new compounds may be used in studies of actin dynamics in living systems. The present invention also relates to methods for preparing such compounds. The synthesis routes combine solid-phase and solution phase peptide synthesis, and has great advantage for efficient preparation of a diverse library of the phalloidin derivatives, especially for the synthesis of phalloidin.

专利号:US-5714597-A
优先权日:1994-07-07
标题:Use of carbocation scavenger during oligonucleotide synthesis
发明人:RAVIKUMAR VASULINGA; ANDRADE MARK; MULVEY DENNIS; COLE DOUGLAS L
权利人:ISIS PHARMACEUTICALS INC
摘要:During the synthesis of oligonucleotides and phosphate linked oligomers, a carbocation scavenging agent is employed to increase the overall yield. The carbocation scavenging agent is used in conjunction with an acidic solution employed during the deprotection step.
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合成参考文献


参考文献:10.1007/s00726-014-1834-8
摘要:Kwak SY, Lee HJ, Yang JK, Lee EJ, Seo M, Lee YS. Antioxidant activity of caffeoyl-prolyl-histidine amide and its effects on PDGF-induced proliferation of vascular smooth muscle cells. Amino Acids. 2014 Dec;46(12):2777–85. doi: 10.1007/s00726-014-1834-8.
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