CAS: 179688-01-8; 7-(Benzyloxy)-6-Methoxyquinazolin-4(3H)-One

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香草酸甲酯置于硝酸,甲酸铵,铁粉,Potassium Carbonate,氯化铵,溶剂黄146体系中,用 乙醇,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 15.0H,反应生成6-甲氧基-7-苄氧基喹唑啉-4-酮
参考文献:新型基于喹唑啉的1,6-萘吡啶酮类化合物作为met抑制剂的结构-活性关系研究具有有效的抗肿瘤功效.
标题:新型基于喹唑啉的1,6-萘吡啶酮类化合物作为met抑制剂的结构-活性关系研究具有有效的抗肿瘤功效.
摘要:作为一种特权的支架,喹唑啉环被广泛用于egfr抑制剂的开发中,而据报道很少有基于喹唑啉的met抑制剂.在我们开发新的以met为靶点的抗癌候选药物的不断努力中,设计,合成了一系列基于喹唑啉的1,6-萘吡啶酮衍生物,并对其生物学活性进行了评估.Sar的初步研究表明,喹唑啉支架对于ii类met抑制剂的a嵌段也是可以接受的.进一步的药代动力学研究导致鉴定出最有前途的化合物22A,具有非常好的体外效价(met,Ic 50 = 9.0 Nm),人微粒体代谢稳定性(t 1/2 = 621.2分钟)和口服生物利用度(f = 42%).此外,22A在met阳性人胶质母细胞瘤u-87 Mg异种移植模型中显示出非常好的体内抗肿瘤功效(75 Mg / Kg中的ir为81%).这些积极的结果表明22A是潜在的针对met的新型抗肿瘤药物铅,值得进一步开发.
Doi:10.1016/j.Ejmech.2020.112785

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