埃罗替尼杂质置于盐酸,过氧乙酸,硫酸,铁粉体系中,用 乙醇 用作溶剂,化学反应 4.0H,反应生成6,7-二甲氧乙氧基喹唑啉-4-酮 参考文献:Facile And Efficient Oxidation Of Quinazolines Into Quinazolin-4(3H)-Ones By Peracetic Acid 标题:Facile And Efficient Oxidation Of Quinazolines Into Quinazolin-4(3H)-Ones By Peracetic Acid 摘要:A New Approach To Synthesize Quinazoline-4(3H)-Ones Was Achieved By Oxidation Of Quinazolines Using Peracetic Acid,Which Possesses Some Advantages Of Economic Reagents,Simplified Operation,High Efficiency,And Environmental Friendliness. Application Of This Method Allowed Us To Synthesize A Series Of Quinazolin-4(3H)-Ones With Different Substituents At 6 And 7 Positions In Good To Excellent Yields,Including The Key Intermediates Of Tyrosine Kinase Inhibitors Such As Pd153035,Erlotinib,And Gefitinib. [supplementary Materials Are Available For This Article. Go To The Publisher'S Online Edition Of Synthetic Communications (R) For The Following Free Supplemental Resource(S): Full Experimental And Spectral Details.] Doi:10.1080/00397911.2013.805230
专利号:US-8133999-B2 优先权日:2003-07-30 标题 :Process for preparation of 6, 7-bis(2-methoxyethoxy) quinazolin-4-one 发明人:NISHINO SHIGEYOSHI; HIROTSU KENJI; SHIMA HIDETAKA; ODA HIROYUKI; SUZUKI SHINOBU 权利人:NISHINO SHIGEYOSHI; HIROTSU KENJI; SHIMA HIDETAKA; ODA HIROYUKI; SUZUKI SHINOBU; UBE INDUSTRIES 摘要:6,7-Bis(2-methoxyethoxy)quinazolin-4-one of formula (5) useful in synthesis of an anti-cancer drug can be prepared by a reaction of ethyl 2-amino-4,5-bis(2-methoxyethoxy)benzoate of formula (4) with an orthoformic acid in the presence of an ammonium acetate:
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:WO-2011147102-A1 优先权日:2010-05-28 标题 :Synthetic method for 6,7-substituents-4-aniline quinazoline 发明人:SHIH KAE-SHYANG; HSIEH YU-JUNG; LIU CHING-WEI 权利人:SHYANG JEN BIOTECH CO LTD; SHIH KAE-SHYANG; HSIEH YU-JUNG; LIU CHING-WEI 摘要:A method for the synthesis of 6,7-substituents-4-aniline quinazoline is disclosed, in which 3,4-substituted benzoic acid is used as a starting material and 6,7-substituents-4-aniline quinazoline is produced from it by esterification, O-alkylation, nitration, nitro group reduction, cyclization, and two-in-one reaction of chlorination and amine-substitution, or by esterification, O-alkylation or nitration, hydrolysis-demethylation, esterification, O-alkylation, nitro group reduction, cyclization, and two-in-one reaction of chlorination and amine-substitution.
专利号:WO-2007138612-A2 优先权日:2006-05-25 标题 :A process for synthesis of [6,7-bis-(2-methoxyethoxy)-quinazolin-4- yl]-(3-ethynylphenyl)amine hydrochloride
专利号:CN-104211648-A 优先权日:2014-08-25 标 题 :A kind of synthesis process method of erlotinib intermediate
专利号:CN-102557977-B 优先权日:2010-12-20 标 题 :Synthesis intermediate of erlotinib and preparation method thereof