2-(氰基甲基)苯甲酸置于乙醇,镍,乙酸乙酯体系中,化学反应生成3,4-二氢异喹啉-1(2H)-酮 参考文献:Beiträge Zur Chemie Der Carbinolamine Ii. Synthesen Von Hydroisocarbostyrilen 标题:Beiträge Zur Chemie Der Carbinolamine Ii. Synthesen Von Hydroisocarbostyrilen 摘要: Doi:10.1002/ardp.19582911105
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-2024174698-A1 优先权日:2022-09-23 标题 :Modular synthesis of 1,2-azaborines via ring-opening bn-isostere benzannulation 发明人:DONG GUANGBIN; LYU HAIRONG; CHEN ZHIJIE; WU YIFEI; CHOI SHINYOUNG 权利人:UNIV CHICAGO 摘要:The present disclosure relates generally to 1,2-azaborines and methods of making the same.
专利号:US-2025178999-A1 优先权日:2022-03-18 标 题:One step synthesis of 1-tetralone compounds and uses thereof in the preparation of (+)-tetralone abscisic acid (aba) 发明人:DIDDI NAVEEN; ABRAMS SUZANNE ROBERTA; LAI LEON 权利人:UNIV SASKATCHEWAN 摘要:The present application is related to a process for preparing 1-tetralone compounds such as compounds of Formula I by reacting a,; 3-unsaturated cyclic ketones that comprise two available hydrogens on the y carbon to the carbonyl with acrolein derivatives with heating in the presence of a suitable organic acid, a suitable organic amine base and suitable inert solvent. For example, the 1-tetralone compound is a tetralone derivative of abscisic acid (ABA).
专利号:US-5849691-A 优先权日:1996-02-20 标 题 :Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II 发明人:MAJER PAVEL; COLLINS JACK; GULNIK SERGEI; ERICKSON JOHN 权利人:US HEALTH 摘要:The present invention relates to the design and synthesis of linear and cyclic inhibitors of cathepsin D and plasmepsins I and II. The present invention also relates to the uses of these inhibitors for inhibiting invasion and metastasis of cancerous cells. The present invention further relates to the use of cathepsin D and plasmepsin I and II inhibitors for the prevention and treatment of Alzheimer's disease and malaria.
专利号:US-9050586-B2 优先权日:2012-03-13 标 题:Enantioselective organic anhydride reactions 发明人:CONNON STEPHEN J; TALLON SEAN; CORNAGGIA CLAUDIO; MANONI FRANCESCO; TORRENTE ESTHER 权利人:CONNON STEPHEN J; TALLON SEAN; CORNAGGIA CLAUDIO; MANONI FRANCESCO; TORRENTE ESTHER; PROVOST FELLOWS & SCHOLARS COLLEGE OF THE HOLY UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN 摘要:Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C 4 -C 50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.
专利号:US-6045755-A 优先权日:1997-03-10 标题 :Apparatus and method for combinatorial chemistry synthesis 发明人:LEBL MICHAEL; POKORNY VIT; KRCHNAK VIKTOR 权利人:TREGA BIOSCIENCES INC 摘要:In a first embodiment, this invention includes an integrated robot apparatus for performing combinatorial chemistry synthesis protocols and having interchangeable work-stations, robot arm tools, and reaction vessels and reaction vessel arrays. The work-stations and tools are specialized to perform tasks necessary for the synthesis in a plurality of the reaction vessels grouped in a plurality of the reaction vessel arrays. Preferably, these elements function interchangeably because they have standardized sizes and conformation. The work-stations and tools include those for fluid dispensing or aspirating from individual reaction vessels or from all the reaction vessels in an array simultaneously. The reaction vessels can include, alternatively, stackable, ball-sealed reaction vessels, microtitre-like reaction vessel arrays, arrays of independent reaction vessels, valve-sealed reaction vessels, septum-sealed reaction vessels, and syringe reaction vessels. In alternative embodiments, this invention includes these work-stations, tools, reaction vessels and reaction vessel arrays in various combinations or sub-combinations either for use in partially integrated robots or for manual or standalone use.