专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-2018265547-A1 优先权日:2014-07-18 标 题 :Z-selective olefin metathesis of peptides 发明人:MANGOLD SHANE L; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.
专利号:US-12162957-B2 优先权日:2018-12-08 标 题:Process for the preparation of plecanatide 发明人:ADAK SANDIP; BONTE MANOJ; KULKARNI CHANDRAKANT; SWAMY VEERANARAYANA; JOGDAND NIVRUTTI; GADGIL HIMANSHU 权利人:ENZENE BIOSCIENCES LTD 摘要:A process for the preparation of plecanatide. Specifically, an improved process for preparation of plecanatide using a non-linear solid phase peptide synthesis. In particular, the process for preparation of plecanatide involves solid phase synthesis of peptide fragments of five amino acid units using 2-chlorotrityl chloride (2-ClTrt) resin and eleven amino acid unit using Wang resin.
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:CN-111825742-B 优先权日:2019-04-18 标题:CTPA is used as a special coupling agent for solid-phase synthesis of peptides with amino acid ionic liquids
专利号:WO-2025015659-A1 优先权日:2023-07-18 标题 :Method for synthesizing amide and/or polypeptide by taking transiently protected amino acid as ammonia component 发明人:ZHAO JUNFENG; WANG PENGHUI; LIU TAO 权利人:UNIV GUANGZHOU MEDICAL 摘要:Provided is a method for synthesizing amide and/or polypeptide by taking a transiently protected amino acid as an ammonia component. In the method, an allenone compound is taken as a condensation reagent, a silylating reagent is used for temporarily protecting a carboxyl group of an amino acid or peptide fragment of which amino and carboxyl groups are not protected, then an α-carbonyl alkenyl ester derivative of another molecular carboxylic acid, or amino acid, or a C-terminal carboxyl group of a polypeptide is used together with same to form an amide bond, and then the temporarily protected carboxyl group can be subjected to on-site deprotection under an acidic condition to obtain a target carboxylic acid product, so as to cyclically construct a new amide bond. The allenone condensation agent can effectively avoid racemization, and the 'temporary protection' strategy enables the three-step reaction of 'protection-condensation-deprotection' to be carried out in one pot, so that greatly excessive chemical reagents, time, manpower and energy consumption required when protecting groups are introduced and protecting groups are removed are avoided, thereby improving the step economy and atom economy of polypeptide synthesis.
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合成参考文献
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