CAS: 71989-16-7; (S)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-4-Amino-4-Oxobutanoic Acid

相似化合物

108321-39-7 132388-59-1 132388-68-2

上下游产品

CAS号70-47-3 L-天冬酰胺 | CAS号82911-69-1 9-芴甲基-N-琥珀酰亚胺碳酸酯 | CAS号88744-04-1 9-芴基甲基五氟苯基碳酸酯 | CAS号28920-44-7 9H-fluoren-9-yl... | CAS号132388-59-1 Fm°C-N-三苯甲基-L-天冬酰胺 | CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号86060-99-3 N-芴甲氧羰基-L-天冬氨酰胺五氟苯酯 | CAS号70-47-3 L-天冬酰胺 | CAS号132388-59-1 Fm°C-N-三苯甲基-L-天冬酰胺 | CAS号127273-06-7 S-2-FM°C-氨基-3-氰基丙酸 | CAS号181954-34-7 N2-芴甲氧羰基-L-2,3-二氨基丙酸 | CAS号162558-25-0 N-Fm°C-N'-B°C-L... | CAS号71989-17-8 Fm°C-L-天冬酰胺4-硝基苯酯

Fmoc-N-三苯甲基-L-天冬酰胺置于盐酸体系中,用 水 作为反应溶剂,化学反应 0.17H,反应生成 Fmoc-L-天冬酰胺
参考文献:Fmoc固相肽合成中新的无tfa裂解和最终脱保护:氟代醇中的稀hcl
标题:Fmoc固相肽合成中新的无tfa裂解和最终脱保护:氟代醇中的稀hcl
摘要:描述了一种从树脂上裂解并去除酸不稳定的保护基以用于fmoc固相肽合成的新方法.在六氟异丙醇或三氟乙醇中的0.1 N Hcl干净并迅速除去叔丁酯和醚,B°C,三苯甲基和pbf基团,并裂解常见的树脂连接基:Wang,Hmpa,Rink酰胺和pal.仅添加5-10%的氢键溶剂会大大阻碍甚至完全抑制反应.但是,可以容忍非氢键溶剂.
DOI:10.1021/ol303124R

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-6316593-B1
优先权日:1996-02-09
标题:Synthesis of VIP analog
发明人：BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M
权利人:HOFFMANN LA ROCHE
摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.

专利号:US-5565606-A
优先权日:1986-10-21
标 题:Synthesis of peptide aminoalkylamides and peptide hydrazides by the solid-phase method
发明人：BREIPHOL GERHARD; KNOLLE JOCHEN
权利人:HOECHST AG
摘要:The invention relates to compounds of the formula I in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y1, Y2, Y3 and Y4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes -[CH2]n- or -O-[CH2]n-, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.