L-丝氨酸置于盐酸,氯化亚砜,Lithium Hydroxide体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 20.17H,以32.6 G的收率获得3-氯-L-丙氨酸 参考文献:Processes For Producing &bgr;-Halogeno-&agr;-Amino-Carboxylic Acids And Phenylcysteine Derivatives And Intermediates Thereof 标题:Processes For Producing &bgr;-Halogeno-&agr;-Amino-Carboxylic Acids And Phenylcysteine Derivatives And Intermediates Thereof 摘要:提供一种在工业上有利的生产β-卤代-α-氨基羧酸的方法.还提供了生产具有高光学纯度的n-保护-S-苯基半胱氨酸及其中间体的方法,其中利用了上述生产方法.公开了一种生产β-卤代-α-氨基羧酸或其盐的方法,包括使用酸和卤化试剂卤化β-羟基-α-氨基羧酸(其中α-位置的氨基基团的碱性未被氨基基团上的取代基掩盖)或其盐.还公开了一种生产由通式(3)表示的具有光学活性的n-保护-S-苯基半胱氨酸或其盐的方法,其中包括将上述生产方法应用于光学活性丝氨酸或其盐,然后在碱性条件下进行氨基保护剂处理和与硫苯酚反应.
专利号:US-10087221-B2 优先权日:2013-03-21 标题 :Synthesis of hydantoin containing peptide products 发明人:HENKEL BERND 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.
专利号:US-7781488-B2 优先权日:2002-06-10 标 题:Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation 发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:WO-2025132814-A1 优先权日:2023-12-21 标 题:Novel synthesis of methyl-2-fluoroacrylate 发明人:BRUNKE JESSICA; FISCHER MICHAEL; WÖSSNER JAN STEPHAN 权利人:VIFOR INT AG 摘要:The present invention relates to novel synthesis methods of methyl 2-fluoroacrylate (MFA) which is a key precursor for the production of Veltassa® (Patiromer). The methods according to the invention are conducted by reacting an α-substituted β-hydroxy propionic acid derivative (I) via one or more intermediate steps involving one or more α-, β-substituted propionic acid derivatives (II) to obtain MFA (III).
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-5200526-A 优先权日:1987-04-27 标题:Syntheses of optically pure α-amino acids from 3-amino-2-oxetanone salts 发明人:ARNOLD LEE D; VEDERAS JOHN C 权利人:UNIV ALBERTA 摘要:A process for the preparation of optically pure α-amino acids comprising the nucleophilic ring-opening of 3-amino-2-oxetanone salts. N-Protected serine β-lactones are deprotected to form heretofore unknown 3-amino-2-oxetanone and its corresponding salts. In turn these previously unknown 3-amino-2-oxetanone salts may be used in the synthesis of other novel or rare stereochemically-pure free amino acids.
专利号:US-7083952-B2 优先权日:2000-03-01 标题 :Nucleotide sequences coding for proteins involved in the biosynthesis of L-serine, an improved method for the microbial production of L-serine and a genetically modified microorganism suitable therefor 发明人:ZIEGLER PETRA; EGGELING LOTHAR; SAHM HERMANN; PETERS-WENDISCH PETRA 权利人:FORSCHUNGSZENTRUM JUELICH GMBH 摘要:The present invention relates to nucleotide sequences of coryneform bacteria, coding for proteins involved in the bio-synthesis of L-serine and to methods for the isolation thereof. The invention further relates to an improved method for the production of L-serine. In addition, the present invention relates to the use of L-serine in the food, animal feed and/or pharmaceutical industries or in human medicine.
[参考文献]: β-Chloro-L-Alanine Can Inhibits Threonine Deaminase, The Branched-Chain Amino Acid Transaminase (Transaminase B), L-Aspartate-Pdecarboxylase, Alanine Racemase And Probably O-Acetylserine Sulfhydrylase. β-Chloro-L-Alanine Reversibly Inhibits The Escherichia Coli
合成参考文献
摘要:Hollmann, F., Science of Synthesis Knowledge Updates, (2021) 3, 437. 参考文献:10.1186/gm404 摘要:Louie RJ, Guo J, Rodgers JW, White R, Shah N, Pagant S, Kim P, Livstone M, Dolinski K, McKinney BA, Hong J, Sorscher EJ, Bryan J, Miller EA, Hartman JL. A yeast phenomic model for the gene interaction network modulating CFTR-ΔF508 protein biogenesis. Genome Med. 2012 Dec 27;4(12):103. 参考文献:10.1016/s0014-5793(02)02958-7 摘要:Yoshimura M, Nakano Y, Fukamachi H, Koga T. 3‐Chloro‐DL‐alanine resistance by L‐methionine‐α‐deamino‐γ‐mercaptomethane‐lyase activity. FEBS Letters. 2002 Jun 21;523(1-3):119–22. doi: 10.1016/s0014-5793(02)02958-7.