CAS: 135248-89-4; (R)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-Mercaptopropanoic Acid

相似化合物

157355-80-1 10318-18-0 20887-95-0

上下游产品

Fmoc-Cys-Oh 157355-77-6
Fmoc-胱氨酸 N-Fmoc-L-Cystine 135273-01-7
N-Fmoc-S-三苯甲基-D-半胱氨酸 Fmoc-D-Cys(Trt)-Oh 167015-11-4
Fmoc-S-三苯甲基-L-半胱氨酸 N-(9-Fluorenylmethoxycarbonyl)-S-Trityl-L-Cysteine 103213-32-7
Fmoc-L-Cys(S-Dmp)-Oh 1403834-73-0
氯甲酸-9-芴基甲酯 (Fluorenylmethoxy)Carbonyl Chloride 28920-43-6
9-芴甲基-N-琥珀酰亚胺基碳酸酯 N-(9H-Fluoren-2-Ylmethoxycarbonyloxy)Succinimide 82911-69-1
(S)-{{7-[bis(Carboxymethyl)Amino]Coumarin-4-Yl}Methyloxycarbonyl}-N-Fmoc-L-Cysteine 1031721-24-0 1-[(9-Fluorenylmethyloxycarbonyl)]Benzotriazole 1131148-55-4

📜Fmoc-L-Cys(Thp)-Oh置于盐酸体系中,用 1,4-二氧六环 用作溶剂,化学反应 2.0H,以99%的收率获得芴甲氧羰基-L-半胱氨酸
参考文献:四氢吡喃基,Fmoc肽化学的一种非芳香族酸不稳定的半胱氨酸保护基
标题:四氢吡喃基,Fmoc肽化学的一种非芳香族酸不稳定的半胱氨酸保护基
摘要:四氢吡喃基(thp),其利用的是一个概念小号,ö-Acetal非芳香族保护基为半胱氨酸,已被证明优于trt,Dpm,Acm,和s吨在使用fmoc固相肽合成bu / T Bu策略.因此,当cys被thp保护时,Cys外消旋作用和c末端3-(1-哌啶基)丙氨酸的形成被最小化.该非芳族保护基团还改善了含cys的被保护肽的溶解性.
Doi:10.1021/acs.Orglett.5B00444

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-7691968-B2
优先权日:2002-05-03
标题:Process for the synthesis of peptides amides by side-chain attachment to a solid phase
发明人：EVANS DAVID JOHN; SIMPKIN DEAN STEVEN ANTHONY; WELLINGS DONALD ALFRED; ATHERTON ERIC
权利人:AVECIA BIOLOG LTD
摘要:A process is provided for the solid-phase synthesis of a peptide amide which comprises attaching an α-nitrogen protected Cα-carboxamide amino acid to a solid support by its side chain, removing the α-nitrogen protecting group, assembling a peptide chain on said α-nitrogen and then cleaving the assembled peptide amide from the solid support. Novel amino acid analogues, peptide amides and solid-phase supports are also provided.

专利号:US-2023220001-A1
优先权日:2020-06-09
标 题:Method for synthesis of thioether-containing peptides
发明人：GRUSS HENDRIK; LUTZ CHRISTIAN; SÃœSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI
权利人:HEIDELBERG PHARMA RES GMBH
摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.