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:US-5166394-A 优先权日:1990-05-23 标题 :Coupling reagent for peptide synthesis 发明人:BREIPOHL GERHARD; KOENIG WOLFGANG 权利人:HOECHST AG 摘要:Novel compounds of the formula I ##STR1## in which X is an anion, and a process for the preparation thereof, are described. Compounds of the formula I are used as coupling reagents in 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
参考文献:10.1007/bf00119994 摘要:Rovero P, Viganò S, Pegoraro S, Quartara L. Synthesis of the bradykinin B1 antagonist [desArg10]HOE 140 on 2-chlorotrityl resin. International Journal of Peptide Research and Therapeutics. 1996 Feb;2(6):319–23. doi: 10.1007/bf00119994.