CAS: 736992-21-5; L-Phenylalaninamide, D-Arginyl-2,6-Dimethyl-L-Tyrosyl-L-Lysyl-

该化合物是合成的丙酸,由氨基酸序列组成,这些元素是蛋白质的构件.该化合物的成分包括L-和D-氨基酸,这可以影响其生物活动和稳定性.苯丙烯,,乙酰,乙酰胺和甘油的存在表明在各种生物化学过程中可能发挥的作用,包括...

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    Nα-Benzyloxycarbonyl-Lysyl(Nε-T-Butyloxycarbonyl)Phenylalaninamide 17337-68-7

    合成工艺路线路线简述

      2',6'-二甲基-L-酪氨酸置于palladium 10% On Activated Carbon,氢气,碳酸氢钠,1-羟基苯并三唑,1-丙基磷酸酐,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,乙酰氯,Lithium Hydroxide体系中,用 1,4-二氧六环,甲醇,二氯甲烷,水,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,40.0 °C,101.33 Kpa 条件下,反应 58.42H,反应生成 D-精氨酰-2,6-二甲基-L-酪氨酰-L-赖氨酰-L-苯丙氨酰胺
      参考文献: Processes For Preparing Pharmaceutically Relevant Peptides[fr] Méthodes De Préparation De Peptides Pertinents Sur Le Plan Pharmaceutique
      标题: Processes For Preparing Pharmaceutically Relevant Peptides[fr] Méthodes De Préparation De Peptides Pertinents Sur Le Plan Pharmaceutique
      摘要:目前的技术提供了产生肽,肽的药用可接受盐和中间体的方法.在某些实施例中,该肽为d-Arg-2´6´-Dmt-Lys-Phe-Nh2.

      海关参考信息

      专利信息


      专利号:US-12018094-B2
      优先权日:2018-04-02
      标 题 :Crystalline dipeptides useful in the synthesis of elamipretide
      发明人:DUNCAN SCOTT M; REDMON MARTIN P
      权利人:STEALTH BIOTHERAPEUTICS INC
      摘要:Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

      专利号:US-10961273-B2
      优先权日:2016-08-16
      标 题 :N-carboxyanhydride-based-scale synthesis of elamipretide
      发明人:DUNCAN SCOTT M; OUDENES JAN; ANDERSEN MARC W
      权利人:STEALTH BIOTHERAPEUTICS CORP
      摘要:Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.

      专利号:US-10112976-B2
      优先权日:2014-06-30
      标 题:Process for the production of D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide
      发明人:ZHAO XINJUN; ZHENG MINYU; YU XIAOZHONG; GAO HANRONG; CORNILLE FABRICE
      权利人:FLAMMA SPA
      摘要:The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.

      专利号:PT-3774844-T
      优先权日:2018-04-02
      标 题:Crystalline dipeptides useful in the synthesis of elamipretide

      专利号:US-10125164-B2
      优先权日:2014-06-25
      标题:Process for preparing D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide
      发明人:ZHAO XINJUN; ZHENG MINYU; YU XIAOZHONG; GAO HANRONG; CORNILLE FABRICE
      权利人:FLAMMA SPA
      摘要:The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.

      专利号:EP-4219523-A3
      优先权日:2018-04-02
      标题:Crystalline dipeptides useful in the synthesis of elamipretide
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      主要参考文献


      1: Schauer A, Jahn D, Vahle B, Barthel P, Männel A, Fabig G, Linke A, Adams V, Augstein A. Mitochondrial Targeting by Elamipretide Improves Myocardial Bioenergetics Without Translating into Functional Benefits in HFpEF. Int J Mol Sci. 2026 Jan 21;27(2):1060. doi: 10.3390/ijms27021060.
      2: Vieira Neto E, Wang M, Szuminsky AJ, Ferraro L, Basu S, Zhao X, Karunanidhi A, Wang Y, Vockley J. Elamipretide Improves Mitochondrial Function in Mitochondrial Trifunctional Protein-Deficient Mice and Human Fibroblasts. J Inherit Metab Dis. 2026 Jan;49(1):e70132. doi: 10.1002/jimd.70132.
      3: Shirley M. Elamipretide: First Approval. Drugs. 2025 Dec 3. doi: 10.1007/s40265-025-02269-8. Epub ahead of print. 19(6):435-436. doi: 10.5582/ddt.2025.01111. Epub 2025 Nov 20. 83(4):123-125. doi: 10.1093/ajhp/zxaf303. 15(17):2497. doi: 10.3390/ani15172497.

      合成参考文献


      参考文献:10.1186/2046-2395-3-6
      摘要:Dai D, Chiao YA, Marcinek DJ, Szeto HH, Rabinovitch PS. Mitochondrial oxidative stress in aging and healthspan. Longevity & Healthspan. 2014 May 01;3(1):6. doi: 10.1186/2046-2395-3-6.
      参考文献:10.1007/s13539-014-0149-7
      摘要:Morley JE, von Haehling S, Anker SD. Are we closer to having drugs to treat muscle wasting disease J cachexia sarcopenia muscle. 2014 May 28;5(2):83–7. doi: 10.1007/s13539-014-0149-7.
      参考文献:10.1007/s11897-018-0386-8
      摘要:Bhatt KN, Butler J. Myocardial Energetics and Heart Failure: a Review of Recent Therapeutic Trials. Curr Heart Fail Rep. 2018 Jun;15(3):191–7. doi: 10.1007/s11897-018-0386-8.
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