专利号:WO-2023169082-A1 优先权日:2022-10-24 标 题:Synthesis method and application of benzothiadiazole-1-ketone compound and derivative thereof 发明人:YI WEI; ZHOU ZHI; WU LIEXIN 权利人:UNIV GUANGZHOU MEDICAL 摘要:Disclosed in the present invention are a synthesis method and application of a benzoselenazole-1-ketone compound and a derivative thereof. Sulfoximine and the element selenium are used as raw materials, and by means of a rhodium catalysis direct C-H functionalization reaction, synthesis of a series of benzoselenazole-1-ketone compounds is achieved. The solution has the advantages of strong functional group compatibility, wide substrate universality, mild conditions, simple operations, and high efficiency and universality. Meanwhile, sulfoximine and the element selenium are used as initial raw materials, a direct C-H functionalization reaction is carried out, and by means of chiral phosphoric acid, synthesis of the chiral benzoselenazole-1-ketone compound is achieved. The application prospect is good, and a sulfydryl structure in biomacromolecules such as polypeptides, saccharides, drug molecules and proteins can be specifically marked. Good anti-SARS-CoV-2 virus activity is exhibited, a trastuzumab biological conjugate can effectively image HER 2 receptors on the cell surface, displays strong fluorescence, and can be applied to the preparation of an imaging reagent for the HER 2 receptor on the cell surface.
专利号:US-4599198-A 优先权日:1985-08-02 标题 :Intermediates in polypeptide synthesis 发明人:HOOVER DENNIS J 权利人:PFIZER 摘要:Bis(t-butoxycarbonyl) derivatives of phenylalanylhistidine as intermediates in the synthesis of rennin inhibiting polypeptides.
专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-6495693-B2 优先权日:1996-11-22 标题:N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; PORTER WARREN J; THORSETT EUGENE D; WU JING 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6987017-B2 优先权日:1999-07-02 标 题:Methods for producing L-isoleucine 发明人:GUILLOUET STEPHANE; SINSKEY ANTHONY J; RODAL AVITAL A; LESSARD PHILIP A 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention relates, in general, to the over-production of L-isoleucine by nonhuman organisms. More specifically, the present invention relates to methods for producing L-isoleucine comprising: (a) growing a transformed nonhuman organism under conditions that provide for synthesis of L-isoleucine, wherein the nonhuman organism comprises one or more copies of a transgene comprising at least one nucleotide sequence encoding catabolic threonine dehydratase; wherein the L-isoleucine is synthesized by the transformed nonhuman organism, the synthesis being greater than that of the corresponding non-transformed nonhuman organism; and (b) recovering the L-isoleucine from the culture medium in which the transformed nonhuman organism was cultured.
专利号:WO-9845313-A1 优先权日:1997-04-04 标题:Novel uncoupling protein and methods of use 发明人:LARKIN SARAH; MOORE CANDACE; ALBRANDT KEITH; YOUNG ANDREW; BEAUMONT KEVIN 权利人:AMYLIN PHARMACEUTICALS INC; LARKIN SARAH; MOORE CANDACE; ALBRANDT KEITH; YOUNG ANDREW; BEAUMONT KEVIN 摘要:A novel uncoupling protein, which we have designated UCP-3, that is expressed in skeletal muscle and brown adipose tissue (BAT), and nucleic acid molecules which encode for said novel protein, are described. Methods of screening for compounds that regulate the expression and the activity of UCP-3 are described, as well as methods of treating diseases or conditions in which the regulation of thermogenesis or respiratory ATP synthesis is desired. Such conditions include obesity, diabetes, malignant hyperthermia, and fever. The construction of cell lines that express UCP-3 is also described.
参考标题:Synthesis Of Novel Chiral Phenanthroline Ligands And A Copper Complex 作者:Xueyan Yang,Zhipeng Zhang,Jingjing Tang,Jian Li |发布日期:2022.11 摘要:A Novel Class Of Chiral Multidentate Ligands Has Been Designed And Synthesized From The Important Classic Ligand 1,10-Phenanthroline And Amino Acids. The Ligands Were Proven To Be Able To Coordinate With Copper(2+) Ion By The Formation Of A Novel Chiral Copper Complex, The Structure Of Which Was Determined By Single-Crystal X-Ray Diffraction.
合成参考文献
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