2-氨基苯甲酸乙酯置于ammonium Acetate,N,N-二异丙基乙胺体系中,用 甲醇,甲苯 作为反应溶剂,化学反应 6.0H,反应生成 4-氯喹唑啉 参考文献:Discovery Of A Series Of Hydroxamic Acid-Based Microtubule Destabilizing Agents With Potent Antitumor Activity 标题:Discovery Of A Series Of Hydroxamic Acid-Based Microtubule Destabilizing Agents With Potent Antitumor Activity 摘要: DOI:10.1021/acs.Jmedchem.1C01451
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-9815816-B2 优先权日:2005-09-30 标 题 :Chemical process for the synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline 发明人:BLIXT JORGEN; GOLDEN MICHAEL DAVID; HOGAN PHILIP JOHN; MARTIN DAVID MICHAEL GLANVILLE; MONTGOMERY FRANCIS JOSEPH; PATEL ZAKARIYA; PITTAM JOHN DAVID; SEPENDA GEORGE JOSEPH; SQUIRE CHRISTOPHER JOHN; WRIGHT NICHOLAS CARTWRIGHT ALEXANDER 权利人:ASTRAZENECA AB; GENZYME CORP 摘要:The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilizing said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.
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:WO-2015023170-A1 优先权日:2013-08-14 标题 :A method for preparation of erlotinib 发明人:KALVINS IVARS; PONOMARJOVS Jurijs; VARACEVA LARISA; CERNOBROVIJS ALEKSANDRS; LEBEDEVS ANTONS; CERNAKS DMITRIJS 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:A method for the preparation N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)- quinazolin-4-amine (erlotinib) from 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one and 3-aminophenylacetylene in the presence of titanium(IV) chloride and anisole is reported.
专利号:US-7365197-B2 优先权日:2000-12-29 标题 :Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines 发明人:BERGER DAN MAARTEN; BIRNBERG GARY HAROLD; WANG YANONG 权利人:WYETH CORP 摘要:This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.
专利号:US-2019263782-A1 优先权日:2005-09-30 标 题 :Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline