CAS: 130309-37-4; (2S,3As,7As)-1-(((9H-Fluoren-9-yl)Methoxy)Carbonyl)Octahydro-1H-Indole-2-Carboxylic Acid

该化合物是一种受保护的氨酸衍生物,含有硬性八氢丁二醇脚架,在peptide合成和药用化学中很有价值.Fmoc(9-氟氧碳氢化合物)组为地雷功能提供正方位保护,在温和基本条件下能够有选择地进行保护.2级的立体化学学(S-配置)和引信环系统加强了一致性控制,使其对设计受限制的peptide或peptimitimics有用.它与标准固相聚(SPS)协议的兼容性能确保将有效融入复杂的序列.这种化合物对于需要精确的空间定向和稳定性的应用特别有利,例如药物发现和生物活性peptided.

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(fluorenylmethoxy)carbonyl chloride (2S,3aS,7aS)-perhydroindole-2-carboxylic acid 32H48N6O5C32H48N6O5 34H52N6O5C34H52N6O5 D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg

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    专利信息


    专利号:US-2020247841-A1
    优先权日:2017-09-27
    标 题 :Synthesis of icatibant
    发明人:RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha
    权利人:BIOCON LTD
    摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.

    专利号:US-11420997-B2
    优先权日:2018-04-13
    标题:Peptide synthesis method
    发明人:SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE
    权利人:JITSUBO CO LTD
    摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.

    专利号:EP-0413277-B1
    优先权日:1989-08-14
    标题:Peptide antagonists of bradykinin
    发明人:HENKE STEPHAN DR; BREIPOHL GERHARD DR; KNOLLE JOCHEN DR; SCHOELKENS BERNWARD PROF DR; GERHARDS HERMANN DR
    权利人:HOECHST AG
    摘要:Peptides of the formula I A-B-C-E-F-K-(D)-Phe-G-M-F'-I (1> in which A is hydrogen, alkyl, alkanoyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, aryl, aryloyl, arylsulphonyl, heteroaryl or an amino acid, each of which can optionally be substituted, B is a basic amino acid, C is a di- or tripeptide, E is the residue of an aromatic amino acid, F is, independently of one another, an amino acid which is optionally substituted in the side chain or is a direct bond, G is an amino acid, F' is defined as F or can be -NH-(CH2)2-8 or optionally a direct bond, I is -OH, -NH2 or -NHC2H5, and K is a radical -NH-(CH2)1-4-CO- or is a direct bond, act as bradykinin antagonists. Their therapeutic uses comprise all pathological states promoted, induced or assisted by bradykinin and bradykinin-related peptides. The peptides of the formula I are prepared by known methods of peptide synthesis.

    专利号:AU-2018343242-A1
    优先权日:2017-09-27
    标 题 :Synthesis of Icatibant

    专利号:EP-3688009-A1
    优先权日:2017-09-27
    标题:Synthesis of icatibant

    专利号:KR-20200088307-A
    优先权日:2017-09-27
    标 题:Synthesis of Icatibant

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    合成方法参考DOI号:10.1039/c6ob02306a
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