专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-7692016-B2 优先权日:2005-11-25 标 题 :Process for the synthesis of quinoline derivatives 发明人:MADUGULA SREE RAMA MURTY; THALLAPELLY SWAMY; BANDARUPALLY JYOTHIRMAI; YADAV JHILLU SINGH 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides an improved process for the synthesis of quinoline derivatives. More particularly the present invention provides an improved and economical process for the synthesis of quinoline derivatives by the reaction of aniline/substituted anilines using two different catalysts, ferric chloride and zinc chloride in a one-pot set up reaction.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-2023348492-A1 优先权日:2020-05-04 标题:Photochemical synthesis of marmycin analogues through a new photochemical reaction involving carbonyl compounds 发明人:SIVAGURU JAYARAMAN; KANDAPPA SUNIL KUMAR; VALLOLI LAKSHMY KANNADI 权利人:BOWLING GREEN STATE UNIV 摘要:Photochemical reactivity of carbonyl compounds leading to the synthesis of the Marmycin core is described. The photochemical reactivity involves an excited state reaction that provides convenient access to bicyclic compounds. The disclosed reactivity is a new photochemical pathway involving 1,3-dicarbonyl compounds and amines as well as for enaminones.
专利号:US-6248891-B1 优先权日:1997-05-23 标题:Synthesis of acridine derivative multidrug-resistant inhibitors 发明人:SHARP MATTHEW JUDE; MADER CATHERINE J; STRACHAN CALUM 权利人:GLAXO WELLCOME INC 摘要:Synthesis of the MDRI of formula (I) from intermediates of acridone acid of formula (II) and aminophenethyl isoquinoline of formula (III), via steps including coupling and conversion to yield the MDRI of formula (I).
专利号:US-6096853-A 优先权日:1998-12-21 标 题 :Synthesis of phenolic monomers containing imide or diimide moieties and high heat carbonate polymers prepared therefrom 发明人:AMERIK VALENTINA; HOEKS THEODORUS L; LIKIBI PARFAIT JEAN MARIE; NELSON MARK 权利人:GEN ELECTRIC 摘要:A process has been surprisingly discovered that can produce a high heat carbonate polymer (i.e., one with a Tg greater that 150° C.), without the drawbacks encountered in attempts to produce a high heat carbonate polymer. The process of the instant invention comprises the steps of: n (1) reacting an aromatic amine with a dihydric phenol to prepare an aminophenol; n (2) reacting an anhydride or dianhydride with the aminophenol to prepare a phenolic precursor; and n (3) reacting the phenolic precursor with a carbonate precursor to prepare a high heat carbonate polymer.
参考文献:10.1007/s11010-011-0953-8 摘要:Makowska M, Łukowska-Chojnacka E, Wińska P, Kuś A, Bilińska-Chomik A, Bretner M. Design and synthesis of CK2 inhibitors. Molecular and Cellular Biochemistry. 2011 Jul 13;356(1-2):91. doi: 10.1007/s11010-011-0953-8.