专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-8846614-B2 优先权日:2011-08-25 标 题 :Process for the synthesis of 37-mer peptide pramlintide 发明人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL 权利人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL; USV LTD 摘要:A process for the production of pramlintide, a 37-mer peptide, is provided. The synthesis provides a high yield synthesis of the peptide in relatively pure form. Further purification can be achieved by preparative HPLC.
专利号:US-6316593-B1 优先权日:1996-02-09 标题:Synthesis of VIP analog 发明人:BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M 权利人:HOFFMANN LA ROCHE 摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.
专利号:US-5219988-A 优先权日:1989-02-22 标 题 :Gem-diamino derivatives and their use in the synthesis of retro-inverso peptides 发明人:GAZERRO LAURA; PINORI MASSIMO; VERDINI ANTONIO S 权利人:ENIRICERCHE SPA; SCLAVO SPA 摘要:This invention relates to new gem-diamino derivatives of general formula (I) ##STR1## where R is the side chain of an amino acid, of which any functional groups are suitably protected, and n X is an acyl group chosen from the group consisting of 2-nitrobenzoyl, 4-chloro-butyryl, acetoacetyl, 4-bromo-butyryl, (2-nitrophenoxy)-acetyl and 2-methyl-2-(2'-nitro-phenoxy)propionyl, of use in introducing gem-diamino residues into retro-inverso peptides. The invention further relates to a method for the synthesis of retro-inverso peptides in which the gem-diamino residue or residues are introduced using the new compound (I).
专利号:US-5124478-A 优先权日:1987-12-22 标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
专利号:WO-2004113530-A1 优先权日:2003-06-18 标题:Polynucleotide for synthesis of labeled protein 发明人:NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU 权利人:MITSUBISHI CHEM CORP; NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU 摘要:A process for producing a labeled protein, comprising translating a gene template in the presence of a labeled compound having a label portion consisting of a labeled substance and an acceptor portion consisting of a compound capable of binding to the C-terminus of protein synthesized by a translation system. In particular, there are provided a polynucleotide for use in synthesis of labeled protein characterized by having the capability of enhancing labeling efficiency through addition to the 3’ end of a base sequence coding for target protein within the gene template and provided a process for producing a labeled protein that is carried out with the use of the polynucleotide.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144. [参考文献]: April Case, Et Al. Development Of A Mechanism-Based Assay For Tissue Transglutaminase--Results Of A High-Throughput Screen And Discovery Of Inhibitors. Anal Biochem. 2005 Mar 15;338(2):237-44. [参考文献]: C Toniolo, Et Al. Chain-Length Dependence For Secondary Structure Formation Of Homo-Oligopeptides From Epsilon-Tert.-Butyloxycarbonyl-L-Lysine With A Lipophilic C-Terminal Group. Int J Pept Protein Res. 1984 Jan;23(1):47-54. [参考文献]: K Itakura, Et Al. Evidence That Malondialdehyde-Derived Aminoenimine Is Not A Fluorescent Age Pigment. Chem Res Toxicol. 2001 May;14(5):473-5. [参考文献]: Manos Gkikas, Et Al. Well-Defined Homopolypeptides, Copolypeptides, And Hybrids Of Poly(L-Proline). Biomacromolecules. 2011 Jun 13;12(6):2396-406.
合成参考文献
摘要:Kroon, E.; Zarganes Tzitzikas, T.; Neochoritis, C. G.; Dömling, A., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 2, 428. 摘要:La Venia, A.; Kovalová, A.; Vrabel, M., Science of Synthesis, (2021) , 97.