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1. (WO2017049983) PREPARATION METHOD OF COPANLISIB
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.:    WO/2017/049983    International Application No.:    PCT/CN2016/088091
Publication Date: 30.03.2017 International Filing Date: 01.07.2016
IPC:
C07D 493/10 (2006.01), A61K 31/35 (2006.01), A61K 31/381 (2006.01), A61K 31/427 (2006.01), A61K 31/4436 (2006.01), A61P 3/10 (2006.01), A61P 9/10 (2006.01), A61P 3/04 (2006.01)
Applicants: SUZHOU LIXIN PHARMACEUTICAL CO., LTD [CN/CN]; No. 21,Tangxi Road, New District Suzhou, Jiangsu 215000 (CN).
XU, Xuenong [CN/CN]; (CN)
Inventors: XU, Xuenong; (CN).
BAO, Zhijian; (CN).
WANG, Zhe; (CN).
ZHANG, Wenjian; (CN).
SU, Jian; (CN).
GU, Xinyu; (CN).
XUE, Jia; (CN).
XIE, Lingling; (CN)
Agent: SUZHOU WISTONG INTELLECTUAL PROPERTY AGENCY(COMMON PARTNERSHIP); Room 804, Building 5 Intellectual property concentrated area Xuesen Road 9, Science& Technology Town, New District Suzhou, Jiangsu 215163 (CN)
Priority Data:
201510618067.6 25.09.2015 CN
Title (EN) PREPARATION METHOD OF COPANLISIB
(FR) PROCÉDÉ DE PRÉPARATION DE COPANLISIB
(ZH) 库潘尼西的制备方法
Abstract: front page image
(EN)The invention discloses a preparation method of copanlisib (BAY 80-6946), taking a known compound of a 2-amino-3-methoxy-4-(3-morpholin-4-ylpropoxy)benzonitrile as a starting material, and performing thereon heterocyclization, cyclic condensation, halogenated amination, amidization, or other unit processes. The preparation method requires an easily accessible material and simple technology, and is cost-effective, environmental friendly, and suitable for industrial production.
(FR)L'invention concerne un procédé de préparation de copanlisib (BAY 80-6946), consistant à prendre un composé connu d'un 2-amino-3-méthoxy-4-(3-morpholin-4-ylpropoxy)benzonitrile en tant que matériau de départ, et à mettre en oeuvre sur celui-ci une hétérocyclisation, une condensation cyclique, une amination halogénée, une amidisation ou d'autres procédés unitaires. Le procédé de préparation nécessite un matériau facilement accessible et une technologie simple, et est rentable, respectueux de l'environnement, et approprié pour une production industrielle.
(ZH)本发明揭示了一种库潘尼西(Copanlisib;BAY80-6946)的制备方法,通过已知化合物2-氨基-3-甲氧基-4-(3-吗啉-4-基丙氧基)苯腈为起始原料,经杂环化、缩合环化、卤代胺化以及酰胺化等单元反应,制得目标化合物库潘尼西。该制备方法原料易得,工艺简洁,经济环保,适合工业化生产。
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 (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)