专利号:US-5939304-A 优先权日:1997-06-05 标题:Method for synthesis of anhydrothrombin 发明人:SUZUKI TOYOAKI; HOSOKAWA KAZUYA; NAGATA MASANORI 权利人:FUJIMORI KOGYO CO 摘要:A method for a synthesis of anhydrothrombin is provided which features a short process, an easy procedure, and high yields. n The method comprises n (A) a step of causing an active serine residue site of thrombin to react with an inhibitor, n (B) a step of performing an alkali treatment at a pH of not less than 11, and n (C) a step of performing an operation of recovery, and carries out these steps sequentially in the order mentioned, and is characterized by causing at least the step of performing the operation of recovery to proceed in the presence of at least one compound selected from the group consisting of polyhydric alcohols and saccharides, and a salt or an amphoteric electrolyte.
专利号:US-12054508-B1 优先权日:2019-04-16 标 题 :Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters 发明人:NIU JIA; LIU CHAO; YANG CANGJIE 权利人:THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:WO-9601260-A1 优先权日:1994-07-01 标题 :Pyridonecarboxylic acid derivative, ester thereof, salt thereof, and intermediate for synthesis of these compounds 发明人:FUJITA MASAHIRO; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 权利人:DAINIPPON PHARMACEUTICAL CO; FUJITA MASAHIRO; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester thereof, a salt thereof, and an antibacterial containing these compounds, wherein R represents optionally halogenated cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z or nitrogen; Z represents hydrogen, halogen, lower alkoxy, halogenated lower alkoxy, lower alkyl, halogenated lower alkyl, lower alkoxy-lower alkyl, etc.; X represents hydrogen, halogen, optionally protected amino, lower alkyl, etc.; Y represents hydrogen or halogen; R1 and R2 represent each independently hydrogen, lower alkyl, etc.; R3 represents hydrogen, halogen, lower alkoxy, lower alkoxy-lower alkyl, halogenated lower alkyl, etc.; and n represents an integer of 0 or 1. The invention also relates to a bicyclic amine compound as a direct intermediate for the pyridonecarboxylic acid derivatives.
专利号:US-9284336-B1 优先权日:2014-08-21 标题 :Synthesis of 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate and analogs 发明人:LAALI KENNETH K 权利人:LAALI KENNETH K; UNIV NORTH FLORIDA 摘要:4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate salt was synthesized and isolated. The pentafluorosulfanyl salt was examined in a wide assortment of reactions to form novel SF 5 -bearing alkenes, alkynes, and biaryl derivatives using Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation of the salt furnished the corresponding p-SF 5 —C 6 H 4 X, C 6 H 4 OS(O)(CF 3 )â•?NSO 2 CF 3 , and p-SF 5 —C 6 H 4 —NTf 2 derivatives. The azide derivative p-SF 5 —C 6 H 4 N 3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. Various SF 5 -bearing alkenes were synthesized by coupling reactions using a metal catalyst. Fluorodediazoniation selectively furnished the fluoro derivative p-SF 5 —C 6 H 4 F. Homolytic dediazoniation gave the unsymmetrical biaryls, thus demonstrating the broad utility of pentafluorosulfanyl diazonium salts as building blocks of SF5-aromatics that are in high demand in many branches of chemistry including biomedicine and materials chemistry.
专利号:EP-4026837-A1 优先权日:2021-01-08 标 题:Process for producing 2,5-diamino-2,5-dideoxy-1,4:3,6-dianhydrohexitol 发明人:RUIJING GUO; PIRES RAUL; BEUCK SASKIA; LATORRE MARTINEZ IRENE CRISTINA; PAN XIANGCHENG; WANG QIANYI; YANG SHICHENG; JIANG YUAN 权利人:COVESTRO DEUTSCHLAND AG 摘要:The invention relates to a process for the synthesis of chiral diamines based on renewable resources. More specifically the invention provides a process for synthesis of diaminoisoidide, diaminoisosorbide, and diaminoisomannide, more specifically 2,5-diamino-2,5-dideoxy-1,4:3,6-dianhydrohexitols.
专利号:US-11027027-B2 优先权日:2015-01-30 标 题:Pyridazinoindole compounds and methods for PET imaging 发明人:MANNING H CHARLES; CHEUNG YIU-YIN; BUCK JASON R; LI JUN 权利人:UNIV VANDERBILT 摘要:Embodiments of the invention include a novel synthesis of the translocator protein (TSPO) ligands, and methods of imaging a molecular events. Also disclosed are compounds for treatment of diseases, including cancer.
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合成参考文献
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