5-氨基颉草酸置于镍 Ammonium Hydroxide,Sodium Hydroxide,氨,氢气,氯甲酸乙酯,三乙胺,三氟乙酸酐体系中,用 四氢呋喃,1,4-二氧六环,乙醇 作为反应溶剂,-10.0~50.0 °C,2.07 Mpa 条件下,反应 9.33H,反应生成 N-(5-氨基戊基)氨基甲酸叔丁酯 参考文献:A Convenient And General Method For The Preparation Oftert-Butoxycarbonylaminoalkanenitriles And Their Conversion To Mono-Tert-Butoxycarbonylalkanediamines 标题:A Convenient And General Method For The Preparation Oftert-Butoxycarbonylaminoalkanenitriles And Their Conversion To Mono-Tert-Butoxycarbonylalkanediamines 摘要:介绍了通过在三氟乙酸酐和三乙胺的存在下脱水相应的羧酰胺2(以两步法制备自氨基酸酸)合成叔丁氧羰基氨基烷腈3的新方法.n-Boc-氨基烷腈3在温和条件下很容易转化为单-N-Boc-烷二胺4,避免了n-保护基团的断裂.单保护的烷二胺4是亲和层析中有用的工具. DOI:10.1055/s-1988-27538
专利号:US-2018312463-A1 优先权日:2015-10-22 标题:Synthesis of Cyclohexane Carboxamide Derivatives Useful as Sensates in Consumer Products 发明人:YELM KENNETH EDWARD; WOS JOHN AUGUST; BUNKE GREGORY MARK; FREDERICK HEATH; HAUGHT JOHN CHRISTIAN; HOKE STEVEN HAMILTON; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product.
专利号:US-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
专利号:US-2019031650-A1 优先权日:2016-01-29 标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies 发明人:HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN 权利人:UNIV YALE 摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.
专利号:WO-2009140467-A1 优先权日:2008-05-15 标 题:Oxobenzindolizinoquinolines and uses thereof 发明人:CUSHMAN MARK S; CINELLI MARIS A; MORRELL ANDREW E; POMMIER YVES G 权利人:PURDUE RESEARCH FOUNDATION; CUSHMAN MARK S; US GOV HEALTH & HUMAN SERV; CINELLI MARIS A; MORRELL ANDREW E; POMMIER YVES G 摘要:The synthesis of aromathecins, substituted 12 H -5,l la-diazadibenzo[ b,h ]fluoren- 11 -ones is described. Use of these cytotoxic compounds and pharmaceutical compositions containing them for the treatment of cancer is described. Two novel processes for the synthesis of this system and a series of 14-substituted aromathecins as novel cytotoxic, topoisomerase I poisons are described.
专利号:US-12037641-B2 优先权日:2015-11-20 标题:Modified nucleotide reagents 发明人:SHEN GENE; YUE STEPHEN; SEBO LUBOMIR; BROGLEY LOUIS 权利人:PACIFIC BIOSCIENCES CALIFORNIA INC 摘要:Labeled nucleotide analogs comprising at least one avidin protein, at least one dye-labeled compound, and at least one nucleotide compound are provided. The analogs are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The analogs are detectable with high sensitivity at desirable wavelengths. They contain structural components that modulate the interactions of the analogs with DNA polymerase, thus decreasing photodamage and improving the kinetic and other properties of the analogs in sequencing reactions. Also provided are nucleotide and dye-labeled compounds of the subject analogs, as well as intermediates useful in the preparation of the compounds and analogs. Compositions comprising the compounds, methods of synthesis of the intermediates, compounds, and analogs, and mutant DNA polymerases are also provided.
专利号:WO-2017070418-A1 优先权日:2015-10-22 标 题:Synthesis of cyclohexane carboxamide derivatives useful as sensates in consumer products
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合成参考文献
参考文献:10.1007/s00044-025-03434-0 摘要:Shi R, Zhang P, Chen M, Lu W, Xu M, Zeng H, He J, Wang Y, Lin Y, Liu J. Dual-PROTACs based on natural product derivative potassium dehydrographolide succinate: design, synthesis, and antitumor activity of a novel EGFR degrader. Med Chem Res. 2025 Jun 30;34(8):1695–713. doi: 10.1007/s00044-025-03434-0. 参考文献:10.1007/s10118-025-3413-8 摘要:Tian W, Wang X, Feng D, Li X, Jin Y, Li H, Liu H. Amine-reactive Polymer Platform for Engineering Surface Modification of Next-generation Sequencing Chips. Chin J Polym Sci. 2025 Sep 02;43(11):2030–41. doi: 10.1007/s10118-025-3413-8. 参考文献:10.1007/978-1-4939-2272-7_17 摘要:Tsukiji S, Hamachi I. Ligand-directed tosyl chemistry for selective native protein labeling in vitro, in cells, and in vivo. Methods Mol Biol. 2015;1266():243–63. doi: 10.1007/978-1-4939-2272-7_17.