2-[2-(2-氨乙氧基)乙氧基]乙醇置于2,2,6,6-Tetramethyl-Piperidine-N-Oxyl,Sodium Hypochlorite,碳酸氢钠体系中,用 二氯甲烷,水 用作溶剂,化学反应生成[2-[2-(Fmoc-氨基)乙氧基]乙氧基]乙酸 参考文献:A Convenient Route To Diversely Substituted Icosahedral Closomer Nanoscaffolds 标题:A Convenient Route To Diversely Substituted Icosahedral Closomer Nanoscaffolds 摘要:The Design And Synthesis Of Icosahedral Polyhedral Borane Closomer Motifs Based Upon Carbonate And Carbamate Anchoring Groups For Biomedical Applications Are Described. Dodecacarbamate Closomers Containing Easily Accessible Groups Of Interest At Their Linker Termini Were Synthesized Via Activation Of The B-Oh Vertices As Aryl Carbonates And Their Subsequent Reaction With Primary Amines. Novel Dodecacarbonate Closomers Were Successfully Synthesized For The First Time By Reacting [closo-B(12)(Oh)(12)](2-) With An Excess Of Respective Aryl Chloroformates,Utilizing Relatively Short Reaction Times,Mild Conditions And Simple Purification Strategies,All Of Which Had Previously Presented Difficulties In Closomer Chemistry. This Methodology For The 12-Fold Degenerate Synthesis Of Carbonate And Carbamate Closomers Will Greatly Facilitate Further Exploration Of Closomers As Monodisperse Nanomolecular Delivery Platforms. Doi:10.1021/ja204488P
专利号:US-2019177392-A1 优先权日:2014-09-23 标 题 :Synthesis of glp-1 peptides 发明人:PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS 权利人:NOVETIDE LTD 摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.
专利号:US-11186608-B2 优先权日:2017-12-21 标 题 :Solid phase synthesis of acylated peptides 发明人:SCHOENLEBER RALPH O; LOIDL GUENTHER 权利人:BACHEM HOLDING AG 摘要:The present invention relates to methods and compounds for the solid phase synthesis of peptides carrying a substituent at an amino group of an amino acid side chain.
专利号:US-9006150-B2 优先权日:2004-11-08 标题:Structural nucleic acid guided chemical synthesis 发明人:HANSEN NILS JOKOB VEST; BLAKSKJAER PETER; HANSEN MARGIT HAAHR; PETERSEN LARS KOLSTER; HEITNER TARA RENEE 权利人:HANSEN NILS JOKOB VEST; BLAKSKJAER PETER; HANSEN MARGIT HAAHR; PETERSEN LARS KOLSTER; HEITNER TARA RENEE; VIPERGEN APS 摘要:Disclosed is a composition comprising the nucleic acid and a chemical compound, said composition forming a star structure defining 3 or more stems extending from a reaction center. The stems are formed by a nucleic acid duplex and the chemical compound has been formed in the reaction center as the reaction product of 3 or more chemical groups. The advantage of the composition is that a close proximity is provided between the chemical groups in the reaction center, thereby promoting a reaction. The invention also relates to a method for preparation of the composition. The advantage of the method is that it does not require the pre-synthesis of a large number of templates and that it is not dependent upon codon/anti-codon recognition for an encoded molecule to be formed.
专利号:US-10920258-B2 优先权日:2018-03-09 标题 :Chemo-enzymatic synthesis of semaglutide, liraglutide and GLP-1 发明人:NUIJENS TIMO; TOPLAK ANA; QUAEDFLIEG PETER JAN LEONARD MARIO 权利人:ENZYPEP B V 摘要:A method for synthesizing a peptide having the sequence His-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Gly is disclosed. The method includes enzymatically coupling:n (a) a peptide C-terminal ester or thioester having a first peptide fragment with the sequence His-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-(thio)ester; and (b) a peptide nucleophile having an N-terminally unprotected amine having a second peptide fragment with the sequence H-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Gly; wherein:n X is Ala or an α-amino-isobutyric acid (Aib) residue; Y is Lys, which Lys has a free side-chain ε-amino group or of which Lys the side-chain ε-amino group is protected with a protective group or of which Lys the side-chain ε-amino group is functionalized with an amino acid or another functional group; and Z is Arg or Lys.
专利号:US-12441760-B2 优先权日:2013-08-29 标 题 :Amino diacids containing peptide modifiers 发明人:BARLOS KLEOMENIS; GATOS DIMITRIOS; BARLOS KOSTAS K; VASILEIOU ZOI 权利人:CHEMICAL & BIOPHARMACEUTICAL LABORATORIES OF PATRAS S A 摘要:The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.
专利号:WO-2025052429-A1 优先权日:2023-09-04 标 题 :An improved process for the preparation of tirzepatide 发明人:SIRIPRAGADA MAHENDER RAO; GANDAVADI SUNIL KUMAR; PARUMANCHALA SHAIK SHAVALI; TELAKALA HEMA SUNDARA RAO; SHAIK KALESHA 权利人:NEULAND LABORATORIES LTD 摘要:An improved process for the preparation of Tirzepatide having the chemical structural Formula I. The present invention also relates to the compounds of SEQ ID NO. 1 to 14 or a pharmaceutically acceptable salt thereof for use in the synthesis of Tirzepatide or a pharmaceutically acceptable salt thereof. The present invention further relates to the intermediate compounds of Formulae II to Formulae XVIII and its process of preparation, which are used in the preparation of Tirzepatide or a pharmaceutically acceptable salt thereof.
1: Chen Y, Xia R, Huang Y, Zhao W, Li J, Zhang X, Wang P, Venkataramanan R, Fan J, Xie W, Ma X, Lu B, Li S. An immunostimulatory dual-functional nanocarrier that improves cancer immunochemotherapy. Nat Commun. 2016 Nov 7;7:13443. doi: 10.1038/ncomms13443. 2: Zhao M, Huang Y, Chen Y, Xu J, Li S, Guo X. PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel. Bioconjug Chem. 2016 Sep 21;27(9):2198-205. doi: 10.1021/acs.bioconjchem.6b00415. Epub 2016 Aug 25. doi: 10.1016/j.biomaterials.2015.07.027. Epub 2015 Jul 15. 4: Zhang Y, Huang Y, Zhao W, Lu J, Zhang P, Zhang X, Li J, Gao X, Venkataramanan R, Li S. Fmoc-conjugated PEG-vitamin E2 micelles for tumor-targeted delivery of paclitaxel: enhanced drug-carrier interaction and loading capacity. AAPS J. 2014 Nov;16(6):1282-91. doi: 10.1208/s12248-014-9651-2. Epub 2014 Sep 6.
合成参考文献
参考文献:10.1007/s11418-024-01841-y 摘要:Matsuda K. Macrocyclizing-thioesterases in bacterial non-ribosomal peptide biosynthesis. J Nat Med. 2024 Aug 30;79(1):1–14. doi: 10.1007/s11418-024-01841-y.