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-2024051897-A1 优先权日:2022-07-26 标题:Synthesis of complex 15n-labeled molecules 发明人:DORSHEIMER JULIA; ROVIS TOMISLAV 权利人:UNIV COLUMBIA 摘要:Methods for conversion of a broad range of amines to their 15N isotopic counterparts and the compounds produced thereby.
专利号:US-2025049791-A1 优先权日:2023-08-03 标题:Synthesis of MEK7 Inhibitors and methods of Use Thereof 发明人:SCHEIDT KARL A; KIM DALTON ROBERT; ORR MEGHAN JO 权利人:UNIV NORTHWESTERN 摘要:Disclosed herein are 4-phenoxypyrimidine compounds and derivatives thereof for use as inhibitors of mitogen-activated protein kinase 7 (MEK7). The disclosed compounds and pharmaceutical compositions thereof may be used in methods for treating a disease or disorder associated with MEK7 activity, including cell proliferative diseases and disorders associated with MEK7 activity, such as cancer.
专利号:US-2003092064-A1 优先权日:2001-04-05 标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof 发明人:READER JOHN C 权利人:MILLENNIUM PHARM INC 摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.
专利号:WO-2013027225-A1 优先权日:2011-08-19 标 题:Processes for the preparation of 4-{4-[5(s)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl} morpholin-3-one 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 摘要:The present invention provides simple, eco-friendly, cost-effective, reproducible, robust and industrial processes for the preparation of intermediate compound 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one (II). The present invention also provides novel intermediates and their use in the synthesis of morpholinone oxazolidine derivatives.
专利号:US-6187923-B1 优先权日:1998-11-09 标题 :Process for the synthesis of quinazolinones 发明人:DENER JEFFREY MARK; LY CUONG QUOC 权利人:AXYS ADVANCED TECHNOLOGIES INC 摘要:The present invention provides a process for synthesizing a compound or a library of compounds of Formula 1A and 1B:
[参考文献]: M Nomura, Et Al. (3-Substituted Benzyl)Thiazolidine-2,4-Diones As Structurally New Antihyperglycemic Agents. Bioorg Med Chem Lett. 1999 Feb 22;9(4):533-8.
合成参考文献
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