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
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.
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.