CAS: 116611-64-4; (S)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-(1H-Imidazol-4-yl)Propanoic Acid

相似化合物

109425-51-6 123333-71-1 135610-90-1

上下游产品

CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号71-00-1 L-组氨酸 | CAS号217082-60-5 [Pyr1]-爱帕琳肽-13 | CAS号2489-13-6 Gly-His | CAS号7451-76-5 甘氨酰甘氨酰-L-组氨酸

📜N-Fmoc-N'-三苯甲基-L-组氨酸置于sodium Thiosulfate,Magnesium Iodide体系中,用 2-甲基四氢呋喃 用作溶剂,化学反应 2.5H,以93%的收率获得n-芴甲氧羰基-L-组氨酸
参考文献:Mgi2-化学选择性切割可去除氨基酸保护基:肽合成的新视野
标题:Mgi2-化学选择性切割可去除氨基酸保护基:肽合成的新视野
摘要:在肽合成领域,成功接近合成靶标的关键在于保护基团的相关组合.他们的选择取决于他们的选择性去除条件.我们在这里介绍了肽化学中一些最常用的保护基团在实验裂解条件下的行为,结合了mgi 2和mw辐射,并使用2-Me-thf作为绿色溶剂.在这些实验条件下,可以在肽化学中重新考虑苄氧羰基保护基以及merrifield树脂.
Doi:10.1002/bip.22908

专利信息

专利号:WO-2023030277-A1
优先权日:2021-08-30
标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog
发明人：SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN
权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD
摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.

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-2025197442-A1
优先权日:2023-12-15
标题:Peptide Synthesis in Aqueous Solution
发明人：MA YONG
权利人:MA YONG
摘要:Four linker molecules were designed to attach peptides to various aqueous-compatible polymer solid phases for Solid Phase Peptide Synthesis (SPPS) in aqueous solutions. Linker molecule A is utilized to attach peptides to an anionic exchange resin in an aqueous solution, and linker molecule B is employed for binding peptides to a cationic exchange resin in an aqueous solution. Both anionic and cationic exchange resins are reusable once the peptide synthesis process is completed.Linker molecule C is utilized to connect the peptide to an amino resin, whereas linker molecule D is employed to bind the peptide to a carboxyl resin. Additionally, linker molecule C can serve as a precursor to linker molecule A, and linker molecule D can function as a precursor to linker molecule B.In all four linker molecules, the amino acid (AA) is linked to solid phases through a benzylic ester bond, which can be cleaved under acidic conditions to release the peptide chain at the end of synthesis.A procedure for dissolving hydrophobic molecules was developed to improve the solubility of hydrophobic compounds, specifically focusing on dissolving Fmoc-protected Amino Acids (Fmoc-AA) in an aqueous solution to facilitate Solid Phase Peptide Synthesis (SPPS) in aqueous conditions.