专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:US-7312343-B2 优先权日:2004-06-02 标 题:Synthesis of α-amino-β-alkoxy-carboxylic acid esters 发明人:SCHMID RUDOLF; ZUTTER ULRICH 权利人:HOFFMANN LA ROCHE 摘要:Compounds of formula I n nand a process for the preparation of such compounds are disclosed.
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:WO-2023214577-A1 优先权日:2022-05-02 标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.
专利号:US-4374060-A 优先权日:1981-07-15 标题 :Process for the preparation of cyclic hexapeptide 发明人:NUTT RUTH F 权利人:MERCK & CO INC 摘要:There is disclosed a process for preparing a cyclic hexapeptide somatostatin analog, specifically cyclo (D-Trp-Lys-Val-Phe-N-Me-Ala-Tyr). The cyclic hexapeptide is synthesized in large quantities in a solution synthesis procedure. However, because of the unexpectedly rapid cyclization rate of this compound, conditions have been developed such that a much more concentrated solution, and thus smaller volumes of the reaction medium, may be employed than would be expected.
专利号:CA-2567914-A1 优先权日:2004-06-02 标 题 :Synthesis of amino-alkoxy-heptanoic alkyl ester