CAS: 58438-04-3; Boc-2-Nal-Oh

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CAS号176896-73-4 (S)-2-叔丁氧基羰基氨基-...

Ethyl 2-Acetylamino-2-Cyano-3-(Naphthalen-2-yl)Propanoate置于盐酸,Sodium Hydroxide体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应 32.0H,反应生成 2-[(叔丁氧羰基)氨基]-3-萘-2-基丙酸
参考文献:酮亚甲基假肽类似物作为凝血酶抑制剂的合成及其生物学活性.
标题:酮亚甲基假肽类似物作为凝血酶抑制剂的合成及其生物学活性.
摘要:酮亚甲基假肽类似物aa-Pro-Arg Psi(coch2)gly-Pip,其中aa是d-或l-氨基酸(dpa,β,β-二苯丙氨酸;αnal,α-萘丙氨酸;βnal,β-萘丙氨酸; Fgl,芴基甘氨酸)具有高度亲脂性的侧链和psi(coch2)是酮亚甲基假肽键,已通过修饰的dakin-West反应在非常温和的条件下以高产率使用三肽4直接在其上具有不稳定的官能团合成了高产量侧链.已经进行了对凝血酶抑制的酶促测定.结构-活性关系研究表明,P3位氨基酸的亲脂性侧链对于与凝血酶非极性位点的结合非常重要.在p3位置带有d-Dpa的化合物1A的ki为0.2 Microm,浓度仅高3倍,凝血酶凝血时间就加倍.这些值是相应的d-Phe类似物的约7倍.此外,1A对纤溶酶,Xa因子,尿激酶和激肽释放酶的抑制作用较弱.初步体内试验(3-4千克兔子为动物模型)显示,在1毫克/千克的剂量下,没有可观测到的副作用(血压的变化和血小板在肺中的积聚).
DOI:10.1021/jm00096A010

专利信息

专利号:US-2024218014-A1
优先权日:2022-11-21
标 题:Synthesis of a cyclic peptide
发明人：BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL
权利人:JANSSEN PHARMACEUTICA NV
摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:EP-4622991-A2
优先权日:2022-11-21
标 题:Synthesis of a cyclic peptide