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-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-7713446-B2 优先权日:2004-06-28 标 题:Synthesis of nanofibers of polyaniline and substituted derivatives 发明人:EPSTEIN ARTHUR J; CHIOU NAN-RONG 权利人:OHIO STATE UNIVERISTY 摘要:Novel, simple methods are presented directed to the synthesis of nanofibers of polyaniline and substituted derivatives. The production of these fibers is achieved via various methods by controlling the concentration of aniline monomer or substituted aniline derivatives or an oxidant in the reaction medium and maintaining said concentration at a level much lower than conventional polyaniline synthesis methods. Methods are disclosed relating to the use of a permeable membrane to control the release of a monomer and/or oxidant as well as a bulk polymerization method.
专利号:WO-2015198349-A1 优先权日:2014-06-25 标 题 :A one pot synthesis of 3-substituted quinoline carboxylates and its derivatives 发明人:GADAKH SUNITA KHANDERAO; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a one pot, simple, cost effective and industrially feasible catalytic synthesis of quinolines or substituted quinolines from anilines with yield >80% yield. The present invention also discloses a process for the synthesis of oxolinic acid using quinolines with yield > 45%.
专利号:US-8058477-B2 优先权日:2006-03-21 标 题 :Process for the synthesis of arylamines from the reaction of an aromatic compound with ammonia or a metal amide 发明人:HARTWIG JOHN F; SHEN QILONG 权利人:HARTWIG JOHN F; SHEN QILONG; UNIV YALE 摘要:A catalytic process for the synthesis of aromatic primary amines, reagent compositions for effecting the process, and transition metal complexes useful in the process, are provided.
专利号:US-4500711-A 优先权日:1977-03-21 标 题 :Synthesis of leucovorin 发明人:WISOWATY JAMES C; SWARINGEN ROY A; YEOWELL DAVID A 权利人:BURROUGHS WELLCOME CO 摘要:In the synthesis of calcium leucovorin (calcium 5-formyl-5,6,7,8-tetrahydrofolate), the use of an amine base in the conversion of anhydroleucovorin (5,10-methenyl-5,6,7,8-tetrahydrofolic acid) to leucovorin unexpectedly results in a pure (USP) product directly from the reaction mixture.
摘要:Collier, S. J.; Singh, S. K., Science of Synthesis, (2010) 45, 83. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 97. 摘要:Celik, I.; Hummel, S.; Kirsch, S. F., Science of Synthesis Knowledge Updates, (2019) 1, 15. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 29. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 30.