CAS: 183319-69-9; N-(3-Ethynylphenyl)-6,7-Bis(2-Methoxyethoxy)Quinazolin-4-Amine Hydrochloride

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CAS号54060-30-9 3-氨基苯乙炔 | CAS号183321-74-6 埃罗替尼 | CAS号299912-59-7 3-butyn-2-ol, 4... | CAS号183322-18-1 4-氯-6,7-二(2-甲氧基... | CAS号179688-29-0 6,7-二甲氧乙氧基喹唑啉-4-酮 | CAS号950596-58-4 2-氨基-4,5-双(2-甲氧... | CAS号122-51-0 原甲酸三乙酯 | CAS号179688-26-7 4,5-二(2-甲氧基乙氧基)... | CAS号183321-74-6 埃罗替尼

N-(3-Trimethylsilyl-Ethynyl)-6,7-Bis(2-Methoxyethoxy)-4-Quinolyl-Amine置于盐酸体系中,用 甲醇 用作溶剂,化学反应 1.0H,以90%的收率获得盐酸埃罗替尼
参考文献:厄洛替尼及其衍生物的制备方法
标题:厄洛替尼及其衍生物的制备方法
摘要:本发明公开了厄洛替尼及其衍生物的制备方法.所述制备方法是将化合物ⅱ(当r2=h,化合物ⅱ=6,7-(2-甲氧基-乙氧基)-喹啉-4-胺)与化合物ⅲ(当r1=sime,R3=i,化合物ⅲ=3-三甲基硅乙炔基-碘化苯)在有机溶剂中,在碱和单质铜和/或铜盐的作用下进行偶联反应得到所述厄洛替尼及其衍生物.本发明以单质铜和/或铜盐或钯试剂作为催化反应的基础,通过中间体化合物ⅱ与化合物ⅲ制备n-(3-乙炔苯基)-6,7-二(2-甲氧基乙氧基)-4-喹啉胺盐酸盐(厄洛替尼,ⅰ)及其衍生物,本发明的制备方法原料廉价易得,反应条件温和,副反应少,收率高,对环境污染小,适于工业化生产.

专利信息

专利号:US-9359370-B2
优先权日:2008-07-08
标题 :Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof
发明人：WANG YINXIANG; XIE GUOJIAN; DING LIEMING; TAN FENLAI; HU YUNYAN; HE WEI; HAN BIN; LONG WEI; LIU YONG; Ai haima; DAVIS CHARLES; ZHANG DON
权利人:BETA PHARMA INC
摘要:The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.

专利号:WO-2007138613-A3
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
发明人：CHANDREGOWDA VENKATESHAPPA; RAO GUDAPATI VENKATESWARA; KUSH ANIL KUMAR; REDDY GOUKANAPALLI CHANDRASEKARA
权利人:VITTAL MALLYA SCIENT RES FOUND; CHANDREGOWDA VENKATESHAPPA; RAO GUDAPATI VENKATESWARA; KUSH ANIL KUMAR; REDDY GOUKANAPALLI CHANDRASEKA
摘要:The present invention provides a process for synthesizing [6,7-bis(2-methoxyethoxy)quinazolin-4-yl]-(3-ethynylphenyl)amine hydrochloride (Erlitinib Hydrochloride) having the formula (I) comprising reacting 3,4-dihydroxy benzaldehyde with bromo derivative of ethyl methyl ether to obtain 3,4-bis(2-methoxyethoxy)benzaldehyde having formula (III). This is converted to give 3,4- bis (2-methoxyethoxy)-benzonitrile which on furthur nitration we obtain 4,5- bis (2-methoxyethoxy)-2-nitrobenzonitrile which on nitro reduction we get 2-amino-4,5-bis(2-methoxyethoxy)benzonitrile. Formylation of this compound yields N'-[2-cyano-4,5-bis(2methoxyethoxy)phenyl]-N,N-dimethylformamidine. Coupling of this formamidine with 3-ethynyl aniline gives erlotinib free base. On furthur treatment of this free base with methanolic/ethanolic hydrochloric acid gives us erlotinib hydrochloride.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

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:US-11130764-B2
优先权日:2017-02-17
标题 :Analogs of vincamine and uses thereof
发明人：HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK
权利人:UNIV FLORIDA
摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.