6-硝基藜芦酸置于palladium 10% On Activated Carbon,氢气,三氯氧磷体系中,用 甲醇,乙二醇甲醚 用作溶剂,化学反应 19.0H,反应生成4-氯-6,7-二甲氧基喹唑啉 参考文献:Novel 4-[5-(Substituted-1,2,4-Oxadiazol-3-yl)Phenylamine] Derivatives Of 6,7-Dimethoxy-Quinazolines As Potent Inhibitors Of Vegf Receptors I And Ii 标题:Novel 4-[5-(Substituted-1,2,4-Oxadiazol-3-yl)Phenylamine] Derivatives Of 6,7-Dimethoxy-Quinazolines As Potent Inhibitors Of Vegf Receptors I And Ii 摘要:一系列新颖的6,7-二甲氧基喹唉类4-[5-(取代-1,2,4-噁二唑-3-基)苯胺]衍生物在c-4位置通过多步合成合成.这些新化合物被测试为血管内皮生长因子受体ii(vegfr-2)的抑制剂.许多化合物显示出vegfr-2抑制活性,在htrf酶活性测定中ic50低至0.017 μm.化合物8J表现出非常好的抗菌活性,通过抑制甲氧西林敏感金黄色葡萄球菌(mssa),甲氧西林耐药金黄色葡萄球菌(mrsa)和美国菌种收藏35218大肠杆菌(mic:0.25-16.00 μg/ml)的生长. Doi:10.14233/ajchem.2016.19884
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:WO-2024127343-A1 优先权日:2022-12-16 标 题 :Inhibitors of ectonucleotide pyrophosphatase / phosphodiesterase 1 (enpp-1) 发明人:RAMANARAYANAN GANAPATHY BHOTLA VENKATA; SARAVANAN PERUMAL; SARAVANAN VADIVELU; NAGARAJ KULKARNI 权利人:SRAVATHI AI TECH PRIVATE LIMITED 摘要:The present invention discloses a novel type of highly potent ENPP-1 inhibitors for the treatment of various diseases particularly, cancer. The compounds of the invention have tail, core, and zinc binding portions (ZBP), where the key feature includes positioning of a sulfoximine-type moiety and an amino nitrogen atom specified as G 1 or G 2 fragment in a saturated cyclic ring in the core part. Synthesis of compounds of formula (1), pharmaceutical compositions and use thereof are also disclosed.
专利号:US-8895747-B2 优先权日:2009-07-27 标 题 :Method and substances for preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL 权利人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
专利号:US-2007021436-A1 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
专利号:CA-2611219-A1 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
专利号:AU-2006258056-A1 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