2-甲基丙氨酸置于氯化亚砜体系中,用 甲醇 用作溶剂,以100%的收率获得2-氨基异丁酸甲酯盐酸盐 参考文献:Molecular Assembly Composed Of A Dendrimer Template And Block Polypeptides Through Stereocomplex Formation 标题:Molecular Assembly Composed Of A Dendrimer Template And Block Polypeptides Through Stereocomplex Formation 摘要:第二代聚酰胺胺(pamam)树枝状分子在八个末端带有右旋螺旋,经证实可通过立体复合形成容纳八个左旋螺旋,从而形成直径为13-14纳米,厚度为6纳米的圆盘状分子组装体. Doi:10.1039/c2Cc30926B
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-6441189-B1 优先权日:2000-03-31 标 题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A 权利人:ABBOTT LAB 摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.
专利号:US-9351974-B2 优先权日:2011-11-10 标题 :Substituted pteridinones for the treatment of cancer 发明人:JIN MEIZHONG; KADALBAJOO MRIDULA; LI AN-HU; MULVIHILL MARK J; SIU KAM W; STEINIG ARNO G; WANG JING 权利人:OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula I, as shown below and defined herein: n npharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
专利号:US-2005032187-A1 优先权日:2003-08-01 标题:Novel peptide-forming enzyme, microbe producing the enzyme and method for producing peptide using them 发明人:YOKOZEKI KENZO; SUZUKI SONOKO; HARA SEIICHI; KATAYAMA SATOSHI 权利人:AJINOMOTO KK 摘要:The present invention relates to a novel enzyme that allows peptide to be produced easily, inexpensively and at high yield without going through a complex synthesis method. More particularly, the present invention provides a novel enzyme that catalyzes a peptide-producing reaction from a carboxy component and an amine component, a microbe that produces the enzyme, and a method for inexpensive production of peptides using this enzyme or microbe. The novel enzyme that efficiently produces peptide was discovered from a newly discovered microbe belonging to the genus Empedobacter , and a method was found that allows peptides to be produced inexpensively and easily.
专利号:US-2005032154-A1 优先权日:2002-07-26 标题 :Method for producing tripeptides and/or peptides longer than tripeptides 发明人:YOKOZEKI KENZO; SUZUKI SONOKO; HARA SEIICHI; ABE ISAO 权利人:AJINOMOTO KK 摘要:It is an object of the present invention to provide a method that allows the production of peptides that are equal to or longer than tripeptides easily, inexpensively and at high yield without going through a complex synthesis method. The inventors of the present invention have found a novel enzyme that efficiently produces a peptide from bacteria belonging to the genus Empedobacter or the genus Sphingobacterium . In the present invention, this enzyme is allowed to act on a carboxy component and an amine component to produce peptides that are equal to or longer than tripeptides.
专利号:BR-112021004839-A2 优先权日:2018-09-26 标 题:crystalline forms of n-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2s,3r) ,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl)phenyl)butanamide and methods of its synthesis
[参考文献]: A Gadea, Et Al. Characterization Of Glycine Transport In Cultured Müller Glial Cells From The Retina. Glia. 1999 Jun;26(4):273-9. [参考文献]: J W Tsang, Et Al. Peptide Sweeteners. 6. Structural Studies On The C-Terminal Amino Acid Of L-Aspartyl Dipeptide Sweeteners. J Med Chem. 1984 Dec;27(12):1663-8. [参考文献]: Koichi Kato, Et Al. An Efficient And Expedient Method For The Synthesis Of 11C-Labeled α-Aminoisobutyric Acid: A Tumor Imaging Agent Potentially Useful For Cancer Diagnosis. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2437-40.
合成参考文献
参考文献:10.1055/s-0034-1380434 摘要:Dobrydnev A, Popova M, Saffon-Merceron N, Listunov D, Volovenko Y. Synthesis of the First Representatives of Spiro-1λ6-isothiazolidine-1,1,4-triones. Synthesis. 2015 Jun 25;47(17):2523–8. doi: 10.1055/s-0034-1380434.