专利号:US-10294196-B2 优先权日:2015-11-18 标题:Process for the synthesis of intermediates useful for preparing 1,3,4-triazine derivatives 发明人:XU SHENG; XU YIHUI 权利人:FMC CORP 摘要:A process for the synthesis of 1,3-diethyl 2-(2-methylhydrazinylidene)propanedioate comprising the step of: reacting 2-halosubstituted diethyl malonate or mixtures of 2-halo-substituted diethyl malonates with methylhydrazine or the salt thereof in the presence of an acid catalyst is disclosed. 1,3-diethyl 2-(2-methylhydrazinylidene)propanedioate is an intermediate useful for preparing 1,3,4-triazines.
专利号:US-6825185-B2 优先权日:2000-12-21 标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D 权利人:NITROMED INC 摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-2018334427-A1 优先权日:2015-11-18 标 题 :Process for the Synthesis of Intermediates Useful for Preparing 1,3,4-Triazine Derivatives
专利号:CN-108349868-A 优先权日:2015-11-18 标题:Process for the synthesis of intermediates useful in the preparation of 1,3,4-triazines
专利号:EP-3377470-B1 优先权日:2015-11-18 标题 :Process for the synthesis of intermediates useful for preparing 1,3,4-triazine derivatives
专利号:CN-114736181-B 优先权日:2022-04-28 标 题:Visible light-mediated synthesis of acylated benzofuran derivatives
[参考文献]: Dominik Schuch, Et Al. Reductive And Brominative Termination Of Alkenol Cyclization In Aerobic Cobalt-Catalyzed Reactions. J Am Chem Soc. 2009 Sep 16;131(36):12918-20.
合成参考文献
摘要:March, T. L.; Duggan, P. J., Science of Synthesis Knowledge Updates, (2014) 1, 381. 摘要:Andries-Ulmer, A.; Gulder, T., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 422.