WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2014183560) AFATINIB AND PREPARATION METHOD OF INTERMEDIATE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/183560    International Application No.:    PCT/CN2014/076537
Publication Date: 20.11.2014 International Filing Date: 30.04.2014
IPC:
C07D 405/12 (2006.01)
Applicants: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD [CN/CN]; Room 1305, Building 1, Lianfeng Commercial Plaza, Industrial Park Suzhou, Jiangsu 215000 (CN).
XU, Xuenong [CN/CN]; (CN)
Inventors: XU, Xuenong; (CN)
Agent: SUZHOU WISTONG INTELLECTUAL PROPERTY AGENCY (COMMON PARTNERSHIP); Room 804, Building 5, Xuesen Road 9 Intellectual Property Concentrated Area Science & Technology Town, New District Suzhou, Jiangsu 215163 (CN)
Priority Data:
201310181150.2 16.05.2013 CN
201310181198.3 16.05.2013 CN
201310180650.4 16.05.2013 CN
201310182778.4 16.05.2013 CN
201310180796.9 16.05.2013 CN
Title (EN) AFATINIB AND PREPARATION METHOD OF INTERMEDIATE THEREOF
(FR) AFATINIB ET PROCÉDÉ DE PRÉPARATION D'UN INTERMÉDIAIRE DE CELUI-CI
(ZH) 阿法替尼及其中间体的制备方法
Abstract: front page image
(EN)Disclosed are a compound of 6-amino-7-hydroxy-3,4-dihydroquinazolin-4-one (I) which can be used in the preparation of Afatinib and the preparation method thereof, the method comprising the following steps: using 3-amino-4-hydroxy benzoic acid or 3-amino-4-hydroxy benzoate or 3-amino-4-hydroxy benzamide as raw materials to prepare the target compound (I) via nitration, reduction and cyclization reactions successively. At the same time, the present invention also reveals two synthesis routes which use compound (I) as a raw material to prepare Afatinib. The preparation and use of compound (I) make the synthesis of Afatinib more simple and environmental, and the yield and quality are improved, thus facilitating industrialization.
(FR)L'invention concerne un composé de 6-amino-7-hydroxy-3,4-dihydroquinazolin-4-one (I) qui peut être utilisé pour la préparation d'afatinib et son procédé de préparation, le procédé comprenant les étapes suivantes : l'utilisation d'acide 3-amino-4-hydroxy benzoïque ou de 3-amino-4-hydroxy benzoate ou de 3-amino-4-hydroxy benzamide en tant que matières premières pour préparer le composé cible (I) par des réactions successives de nitration, réduction et cyclisation. La présente invention révèle également simultanément deux voies de synthèse qui utilisent le composé (I) en tant que matière première pour la préparation d'afatinib. La préparation et l'utilisation du composé (I) rendent la synthèse d'afatinib plus simple et plus écologique, et le rendement et la qualité sont améliorés, facilitant ainsi l'industrialisation.
(ZH)本发明揭示了一种可用于阿法替尼(afatinib)制备的化合物6-氨基-7-羟基-3,4-二氢喹唑啉-4-酮(I)及其制备方法,其包括如下步骤:以3-氨基-4-羟基苯甲酸或3-氨基-4-羟基苯甲酸酯或3-氨基-4-羟基苯甲酰胺为原料,依次经硝化、还原以及成环反应,制得目标化合物(I)。同时,本发明还揭示了以化合物(I)为原料,制备阿法替尼的两条合成路线。通过化合物(I)的制备和应用,使阿法替尼的合成更加简洁环保,收率和质量有所提高,利于产业化。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)