CAS: 196603-96-0; 4-((4-Bromo-2-Fluorophenyl)Amino)-6-Methoxyquinazolin-7-Ol

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7-(benzyloxy)-N-(4-bromo-2-fluorophenyl)-6-methoxyquinazolin-4-amine hydr°Chloride 4-bromo-2-fluoroaniline 2-amino-4-benzyloxy-5-methoxybenzamide 7-benzyloxy-6-methoxy-3,4-dihydroquinazolin-4-one N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]quinazoline-4-amine N-(4-bromo-2-fluorophenyl)-7-(3-chloropropoxy)-6-methoxyquinazolin-4-amine 4-(((4-((4-bromo-2-fluorophenyl)amino)-6-methoxyquinazolin-7-yl)oxy)methyl)piperidine-1-carboxylic acid tert-butyl ester (4R,6S)-{6-[4-(4-bromo-2-fluorophenylamino)-6-methoxyquinazolin-7-yloxymethyl]-2,2-dimethyl-[1,3]dioxan-4-yl}-acetic acid ethyl ester

2-氨基-4-苄氧基-5-甲氧基苯甲酰胺置于氯化亚砜,N,N-二甲基甲酰胺,三氟乙酸体系中,用 1,4-二氧六环,异丙醇 用作溶剂,化学反应 31.83H,反应生成4-(4-溴-2-氟苯胺基)-7-羟基-6-甲氧基喹唑啉
参考文献:一类新型有效的vegf受体酪氨酸激酶抑制剂的设计与构效关系.
标题:一类新型有效的vegf受体酪氨酸激酶抑制剂的设计与构效关系.
摘要:合成了一系列取代的4-苯胺基喹唑啉和相关化合物,作为血管内皮生长因子(vegf)受体(flt和kdr)酪氨酸激酶活性的潜在抑制剂.酶筛查表明,对于双环系统而言,存在窄的构效关系(sar),喹唑啉,喹啉和cinnolines具有活性,通常优选喹唑啉和喹啉.对苯胺的取代进行了研究,并清楚地表明,在c-4'位置优选使用较小的亲脂性取代基,例如卤素或甲基.在c-2'位置优选小的取代基,例如氢和氟.在苯胺的间位引入羟基会产生最有效的flt和kdr酪氨酸激酶活性抑制剂,其ic(50)值在纳摩尔范围内(例如10,12,13,16和18).对喹唑啉c-6和c-7位置的研究表明,在c-7可以容忍大范围的取代基,而c-6的变化受到更大的限制.在c-7处,中性,碱性和杂芳族侧链产生非常有效的化合物,如甲氧基乙氧基衍生物13(ic(50)<2 Nm)所示.与与fgf受体相关的抑制剂(50至3800倍)相比,我们的
Doi:10.1021/jm990345W

专利信息

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-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

专利号:US-10344015-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

专利号:US-2014378684-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

专利号:US-8865899-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

专利号:US-2024150317-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