📜喹啉置于tris-(Dibenzylideneacetone)Dipalladium(0),水,Potassium Hydroxide体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 16.0H,以95%的收率获得产物3-羟基喹啉 参考文献:Me3(Ome)Tbuxphos: A Surrogate Ligand For Me4Tbuxphos In Palladium-Catalyzed C-n And C-o Bond-Forming Reactions 标题:Me3(Ome)Tbuxphos: A Surrogate Ligand For Me4Tbuxphos In Palladium-Catalyzed C-n And C-o Bond-Forming Reactions 摘要:A New Biarylphosphine Ligand,Me-3(Ome)Tbuxphos (L3),Was Designed As A Surrogate For Me(4)Tbuxphos (L1). The Me-3(Ome)Tbuxphos Could Be Prepared In A Chromatography-Free Manner From Inexpensive And Readily Available 2,3,6-Trimethylphenol. Comparative Studies Demonstrated That A Catalyst Based On Me-3(Ome)Tbuxphos Displayed The Same Reactivity As A Catalyst Based On Me(4)Tbuxphos For Pd-Catalyzed C-N And C-O Bond-Forming Processes. DOI:10.1021/jo202537E
专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-2004072738-A1 优先权日:2000-12-21 标 题 :Analogues of thiocoraline and be-22179 发明人:BOGER DALE L 摘要:A process for the total synthesis of thiocoraline and BE-22179 establishes the relative and absolute stereochemistry of these compounds and enables the construction and characterization of a series of related analogues. The mechanism for the bioactivity of thiocoraline, BE-22179 and their related analogues is charaterized. Thiocoraline, BE-22179, and their related analogues are disclosed to bind to DNA by high-affinity bisintercalation and are disclosed to exhibit exceptional cytotoxic activity.
专利号:US-11390645-B2 优先权日:2016-08-08 标题:Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene 发明人:BARBIERI FRANCESCO; LENNA ROBERTO 权利人:IND CHIMICA SRL 摘要:A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6).
专利号:EP-0839807-A1 优先权日:1996-10-30 标题:Synthesis of benzo(f)quinolinones
专利号:RU-2749134-C1 优先权日:2016-08-08 标 题:METHOD FOR SYNTHESIS OF 3β-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE
摘要:Pharmaceutical Chemistry Journal, 16(259), 1982 摘要:A. Albert and J. N. Phillips. J. Chem. Soc. 1956, 1294. 摘要:Harnying, W.; Berkessel, A., Science of Synthesis: Knowledge Updates, (2024) 1, 399.