专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
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:WO-2023102600-A1 优先权日:2021-12-06 标题:Synthesis of amphiphilic block copolymers and polymeric nanofibers produced therefrom 发明人:ZETTERLUND PER B; ISHIZUKA FUMI; KIM HYUN JIN; CHATANI SHUNSUKE; NIINO HIROSHI 权利人:NEWSOUTH INNOVATIONS PTY LTD 摘要:The present disclosure relates to the field of synthesis of block copolymers, and polymeric nanofibers having a core-shell morphology produced therefrom. The present disclosure relates to the field of synthesis of block copolymers where one block is more hydrophobic than the other block and is a different composition. The disclosure also relates to uses of these polymeric nanofibers in various applications, such as reinforcing a polymeric matrix and for coatings applications.
专利号:US-5569762-A 优先权日:1994-01-14 标题:Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds 发明人:WISSNER ALLAN; TROVA MICHAEL P 权利人:AMERICAN CYANAMID CO 摘要:The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R 1 , R 50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.
专利号:US-10787458-B2 优先权日:2014-09-25 标 题:Chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-A]pyrazines 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:Disclosed is a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I): n nor a solvate thereof. The novel chiral synthesis avoids the use of protection/deprotection steps.
专利号:US-10918627-B2 优先权日:2016-05-11 标 题:Convergent and enantioselective total synthesis of Communesin analogs 发明人:MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.
摘要:Shi, Y.; Cole-Hamilton, D. J.; Kamer, P. C. J., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 239. 摘要:Liu, G.; Feng, J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 325. 参考文献:10.1021/cc030002q 摘要:Masip I, Ferrándiz-Huertas C, García-Martínez C, Ferragut JA, Ferrer-Montiel A, Messeguer A. Synthesis of a library of 3-oxopiperazinium and perhydro-3-oxo-1,4-diazepinium derivatives and identification of bioactive compounds. J Comb Chem. 2004 Jan;6(1):135–41. doi: 10.1021/cc030002q. 参考文献:10.1021/jo800898k 摘要:Obika S, Yasui Y, Yanada R, Takemoto Y. Concise synthesis of the CDE ring system of tetrahydroisoquinoline alkaloids using carbophilic Lewis acid-catalyzed hydroamidation and oxidative Friedel-Crafts cyclization. J Org Chem. 2008 Jul 04;73(13):5206–9. doi: 10.1021/jo800898k.