CAS: 105047-45-8; Fmoc-Lys-Oh

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(S)-2-((((9H-芴-9-基)甲氧基)羰基)氨基)-6-(((4-甲氧基苯基)二苯基甲基)氨基)己酸置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 1.0H,反应生成Fmoc-赖氨酸
参考文献:微波辅助合成内消旋羧基烷基 Bodipy 及其在荧光成像中的应用
标题:微波辅助合成内消旋羧基烷基 Bodipy 及其在荧光成像中的应用
摘要:在该研究中,公开了一种用于合成具有游离羧酸基团(随后与肽偶联)的模块化内消旋-Bodipy(硼二吡咯亚甲基)衍生物的显着改进方法.该方法提供了一种非常有效的合成路线,其总产率比其他报告高出三倍以上.所得内消旋-Bodipy 酸允许进一步容易地掺入肽中.Meso-Bodipy 肽显示出 495-498 Nm 的最大吸收和 504-506 Nm 的发射最大值,33 383-80 434 M-1 Cm-1的摩尔吸收系数和 0.508-0.849 的荧光量子产率.中观评估了-Bodipy-C(Rgdyk) 肽的血浆稳定性,然后评估其在体内和离体的荧光成像适用性(被证明甚至可以持续长达 4 小时) .由于自发荧光,体内光学成像受到限制,然而,离体组织分析显示 Bodipy-C(Rgdyk) 内化和癌症检测,从而使其成为一种新的肿瘤整合素相关荧光探针,同时显示染料没有干扰该配体结合受体的特性.
Doi:10.1039/d0Ob01415J

专利信息

专利号:US-2008287649-A1
优先权日:2006-12-29
标 题 :Methods for the synthesis of cyclic peptides
发明人：CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.

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: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-11518794-B2
优先权日:2016-08-19
标 题:Synthesis method for liraglutide with low racemate impurity
发明人：FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG
权利人:SHENZHEN JYMED TECH CO LTD
摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.

专利号:US-12251674-B2
优先权日:2012-11-14
标 题:Substrates, systems, and methods for array synthesis and biomolecular analysis
发明人：RAJASEKARAN JOHN J; JAYARAMAN VASANTH; WANG TIANHAO; BEI KANG; KRISHNAMURTHY HARI KRISHNAN; VEDANTHAM PUNITHA
权利人:VIBRANT HOLDINGS LLC
摘要:Disclosed herein are formulations, substrates, and arrays. In certain embodiments, substrates and arrays comprise a porous layer for synthesis and attachment of polymers or biomolecules. Also disclosed herein are methods for manufacturing and using the formulations, substrates, and arrays, including porous arrays. Also disclosed herein are formulations and methods for one-step coupling, e.g., for synthesis of peptides in an N→C orientation. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.