CAS: 1155-64-2; (S)-2-Amino-6-(((Benzyloxy)Carbonyl)Amino)Hexanoic Acid

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L-赖氨酸置于c.I.酸性橙108,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,乙醇 用作溶剂,化学反应 25.05H,反应生成N6-Cbz-L-赖氨酸
参考文献:使用9-Bbn基团作为瞬变保护基团使α-氨基酸的反应链功能化
标题:使用9-Bbn基团作为瞬变保护基团使α-氨基酸的反应链功能化
摘要:摘要 实现化学选择性是化学合成中的长期挑战.已经使用不同的方法解决了这个问题,但是最终的解决方案仍在等待中.例如,在肽化学中,特别是对于具有侧链官能度的氨基酸,其具有与主要功能基团类似的反应模式,例如天冬氨酸和谷氨酸,赖氨酸和鸟氨酸,已经使用了特定的半永久性保护基.使用9-Borabicyclo [3.3.1]壬烷(9-Bbn-H)作为瞬时保护基团以选择性保护α-氨基酸,从而可以对嵌入在其侧链中的官能团进行化学选择性处理.分子,描述. 实现化学选择性是化学合成中的长期挑战.已经使用不同的方法解决了这个问题,但是最终的解决方案仍在等待中.例如,在肽化学中,特别是对于具有侧链官能度的氨基酸,其具有与主要功能基团类似的反应模式,例如天冬氨酸和谷氨酸,赖氨酸和鸟氨酸,已经使用了特定的半永久性保护基.使用9-Borabicyclo [3.3.1]壬烷(9-Bbn-H)作为瞬时保护基团以选择性保护α-
Doi:10.1055/s-0032-1316848

专利信息

专利号:US-6166217-A
优先权日:1998-02-09
标题 :Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril
发明人：CANNATA VINCENZO; MERLI VALERIANO; SAGUATTI STEFANO
权利人:ALLIED SIGNAL INC
摘要:Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.

专利号:US-4105652-A
优先权日:1977-08-05
标 题 :Synthesis of human β-endorphin
发明人：MEIENHOFER JOHANNES ARNOLD; WANG SU-SUN
权利人:HOFFMANN LA ROCHE
摘要:Human β-endorphin (β h -endorphin) is prepared by solution phase peptide synthesis. Synthesis proceeded via the protected β-endorphin fragments 1-9, 10-18, 19-21 and 22-31.

专利号:US-8455619-B2
优先权日:2008-11-25
标 题 :Polypeptide synthesis for drug delivery
发明人：LATHAM KEITH R
权利人:LATHAM KEITH R
摘要:The present invention provides improved methods for the synthesis of polypeptide or peptide-linked compounds via a NCA-based polymerization reaction that produces high product yields in much less time. Such improved methods are achieved by application of a higher temperature and/or reduced pressure to the reaction such that an NCA-containing monomer melts.

专利号:US-8217142-B2
优先权日:1996-07-17
标题 :Liquid phase peptide synthesis of KL-4 pulmonary surfactant
发明人：ABDEL-MAGID AHMED F; EGGMANN URS; MARYANOFF CYNTHIA ANNE; THALER ADRIAN; VILLANI FRANK J
权利人:ABDEL-MAGID AHMED F; EGGMANN URS; MARYANOFF CYNTHIA ANNE; THALER ADRIAN; VILLANI FRANK J; ORTHO PHARMA CORP
摘要:The invention relates to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu 4 ) 4 -Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the α-carbon.

专利号:US-4772587-A
优先权日:1985-04-16
标题:Dipeptide derivative of fatty acid
发明人：TANAKA TAKAHARU; HIGUCHI NAOKI; SAITOH MASAYUKI; HASHIMOTO MASAKI
权利人:SUNTORY LTD
摘要:A novel compound that exhibits inhibitory activity against prolyl endopeptidase and a method for chemical synthesis of said compound, as well as its use as a prolyl endopeptidase inhibitor and an anti-amnesic agent that contains said compound as the active ingredient are provided.

专利号:US-6664368-B1
优先权日:1997-11-27
标题:Inhibition of nuclear import by backbone cyclic peptide analogs
发明人：FRIEDLER ASSAF; LOYTER ABRAHAM; GILON CHAIM; WOLF AMNON
权利人:YISSUM RES DEV CO; PEPTOR LTD
摘要:The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention are exemplified for the NLS sequences of the human immunodeficiency virus type 1 proteins MA, Vpr, Tat and NLS-like sequences of HIV-1 protein Vif. We disclose the discovery of a novel, highly potent backbone cyclic peptide, designated BCvir, which inhibits nuclear import with an IC50 value of 35 nM. This inhibitory potency is to be compared to 12 muM exhibited by the linear parent HIV-1 MA NLS peptide. BCvir also reduced HIV-1 production by 75% in infected non-dividing cultured human T-cells and was relatively resistant to tryptic digestion. These properties render backbone cyclic peptide analogs of NLS or NLS-like sequences as candidates for novel drugs based on blocking nuclear import of viral genomes.