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1. (WO2017016410) PREPARATION METHOD FOR ANTITUMOR DRUG AP26113
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/016410 International Application No.: PCT/CN2016/090408
Publication Date: 02.02.2017 International Filing Date: 19.07.2016
IPC:
C07F 9/6558 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6558
containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
Applicants:
苏州明锐医药科技有限公司 SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD [CN/CN]; 中国江苏省苏州市 工业园区联丰商业广场1幢1305室 Room 1305, Building 1,Lianfeng Commercial Plaza, Industrial District Suzhou, Jiangsu 215000, CN
Inventors:
许学农 XU, Xuenong; CN
Agent:
苏州慧通知识产权代理事务所(普通合伙) SUZHOU WISTONG INTELLECTUAL PROPERTY AGENCY(COMMON PARTNERSHIP); 中国江苏省苏州市 高新区科技城学森路9号知识产权集聚区5号楼804室 Room 804, Building 5 Intellectual Property Concentrated Area,Xuesen Road 9,Science& Technology Town, New District Suzhou, Jiangsu 215163, CN
Priority Data:
201510444071527.07.2015CN
Title (EN) PREPARATION METHOD FOR ANTITUMOR DRUG AP26113
(FR) PROCÉDÉ DE PRÉPARATION D’UN MÉDICAMENT ANTITUMORAL AP26113
(ZH) 抗肿瘤药物AP26113的制备方法
Abstract:
(EN) Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4-[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4-[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4-[4-(dimethyl amino)piperid-1-yl]aniline]guanidine by means of a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally-friendly, and suitable for industrial production.
(FR) La présente invention concerne un procédé de préparation d’un médicament antitumoral AP26113 (I). Le procédé comprend les étapes de préparation suivantes : cyclisation de N-[2-méthoxyl-4-[4-(diméthyl amino)pipérid-1-yl]aniline]guanidine et de N,N-diméthylamino acrylate, condensation de N-[2-méthoxyl-4-[4-(diméthyl amino)pipérid-1-yl]aniline]guanidine et de 4-(diméthyl phosphitylate)aniline, et chloration de N-[2-méthoxyl-4-[4-(diméthyl amino)pipérid-1-yl]aniline]guanidine à l’aide d’un agent de chloration, de manière séquentielle, afin de préparer de l’AP26113 (I). Le procédé de préparation adopte des matières premières facilement obtenues, entraîne peu de réactions latérales, et est économique, écologique, et convient à la production industrielle.
(ZH) 本发明揭示了一种抗肿瘤药物AP26113(I)的制备方法,其制备步骤包括:N-[2-甲氧基-4-[4-(二甲基氨基)哌啶-1-基]苯胺]胍依次与N,N-二甲氨基丙烯酸酯、4-(二甲基亚磷酰)苯胺和氯化剂发生环合反应、缩合反应以及氯化反应制得AP26113(I)。该制备方法原料易得,副反应少,经济环保,适合工业化生产。
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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, 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 (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, 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)