CAS: 77284-32-3; Fmoc-Nle-Oh

相似化合物

112883-41-7 112883-42-8 15027-14-2

上下游产品

2-N-fluorenylmethoxycarbonylaminohex-4-enoic acid (fluorenylmethoxy)carbonyl chloride L-Norleucine Fm°C-norleucineFm°C-Nle-OTDO Fm°C-Nle-OBg

2-N-Fluorenylmethoxycarbonylaminohex-4-Enoic Acid置于氢气体系中,用 甲醇 作为反应溶剂,20.0 °C,413.69 Kpa 条件下,以105 Mg的收率获得产物芴甲氧羰酰基正亮氨酸
参考文献:串联钌-亚烷基催化的交叉复分解/氢化:亲脂氨基酸的合成.
标题:串联钌-亚烷基催化的交叉复分解/氢化:亲脂氨基酸的合成.
摘要:脂质氨基酸的高效合成可以通过ru-亚烷基催化的长链烯烃与市售的烯丙基甘氨酸的交叉复分解反应实现.然后可以通过使用废复分解催化剂在温和的反应条件下任选地将所得的不饱和类似物氢化.版权所有©2013欧洲多肽协会和john Wiley&sons,Ltd.
DOI:10.1002/psc.2522

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-2024018099-A1
优先权日:2020-11-19
标题 :Synthesis of prostate specific membrane antigen (psma) ligands
发明人：ANDREAE FRITZ
权利人:NOVARTIS AG
摘要:The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.