📜L-苯基丙氨酸叔丁酯置于ethyl Azodicarboxylate,氢溴酸,溶剂黄146,三苯基膦体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,反应生成N-甲基-L-苯丙氨酸 参考文献:Pmc-Protected Amino Acid Esters As Substrates In N-Alkylamino Acid Synthesis 标题:Pmc-Protected Amino Acid Esters As Substrates In N-Alkylamino Acid Synthesis 摘要:N-Alkylamino Acids May Be Synthesised Via Mitsunobu Reaction Of N-(2,2,5,7,8-Pentamethylchroman-6-Sulphonyl-)-Amino Acid Esters With Various Alcohols And Subsequent Deprotection. Copyright (C) 1996 Published By Elsevier Science Ltd Doi:10.1016/s0040-4039(96)02350-7
专利号:US-2023272006-A1 优先权日:2021-08-31 标题:Peptidomimetics and method of synthesis thereof 发明人:NEFZI ADEL 权利人:NEFZI ADEL; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides compounds, peptidomimetics, and methods of synthesis thereof. The subject invention provides the synthesis and use of guanidino acids and/or poly guanidino acids not only as vehicles for drug delivery but as toolbox for drug discovery. The peptidomimetic of the subject invention comprises oligo(guanidino acid)s or poly(guanidino acid)s with guanidines as peptide bond surrogates. The incorporation of the guanidine as amide bond surrogates offers significant differences in polarity, hydrogen bonding capability, and acid-base character.
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:WO-2008098280-A1 优先权日:2007-02-16 标题:Methods for the synthesis of dicarba bridges in growth hormone peptides 发明人:ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 权利人:POLYCHIP PHARMACEUTICALS PTY; UNIV MONASH; ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 摘要:The invention relates to peptides comprising the carboxy terminal sequence of a growth hormone or an analogue of such a peptide in which the disulfide bridge is replaced by a dicarba bridge. Compositions containing such dicarba bridged peptides and method of treating obesity in an animal such as a human comprising administration of such dicarba bridged peptides are also disclosed.
专利号:US-7635749-B2 优先权日:1999-12-24 标题 :Methods and compositions for prolonging elimination half-times of bioactive compounds 发明人:DENNIS MARK S; LOWMAN HENRY B; DELANO WARREN L 权利人:GENENTECH INC 摘要:Peptide ligands having affinity for IgG or for serum albumin are disclosed. Also disclosed are hybrid molecules comprising a peptide ligand domain and an active domain. The active domain may comprise any molecule having utility as a therapeutic or diagnostic agent The hybrid molecules of the invention may be prepared using any of a number techniques including production in and purification from recombinant organisms transformed or transfected with an isolated nucleic acid encoding the hybrid molecule, or by chemical synthesis of the hybrid. The hybrid molecules have utility as agents to alter the elimination half-times of active domain molecules. Elimination half-time is altered by generating a hybrid molecule of the present invention wherein the peptide ligand has binding affinity for a plasma protein. In a preferred embodiment, a bioactive molecule having a short elimination half-time is incorporated as or into an active domain of the hybrid molecules of the invention, and the binding affinity of the peptide ligand domain prolongs the elimination half-time of the hybrid as compared to that of the bioactive molecule.
专利号:US-6596692-B1 优先权日:2000-07-31 标 题 :Substance P analogs for the treatment of cancer 发明人:BURMAN ANAND C; PRASAD SUDHANAND; MUKHERJEE RAMA; JAGGI MANU; SINGH ANU T 权利人:DABUR RES FOUNDATION 摘要:The present invention encompasses novel synthetic peptide analogs that are antagonists to Substance P, substance P like peptides and related peptides and are useful for the treatment of cancer. The invention particularly relates to the design and synthesis of the novel substance P antagonist analogs incorporating alpha,alpha-dialkylated amino acids in a site specific manner. The invention encompasses methods for the generation of these peptides, compositions containing these peptides and pharmacological applications of these peptides specifically in the treatment and prevention of cancer.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.