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

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)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
35
having six-membered rings with one oxygen as the only ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
38
having sulfur as a ring hetero atom
381
having five-membered rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
427
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4436
containing a heterocyclic ring having sulfur as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
Applicants:
苏州立新制药有限公司 SUZHOU LIXIN PHARMACEUTICAL CO., LTD [CN/CN]; 中国江苏省苏州市 高新区塘西路21号 No. 21,Tangxi Road, New District Suzhou, Jiangsu 215000, CN
许学农 XU, Xuenong [CN/CN]; CN
Inventors:
许学农 XU, Xuenong; CN
包志坚 BAO, Zhijian; CN
王喆 WANG, Zhe; CN
张文件 ZHANG, Wenjian; CN
苏健 SU, Jian; CN
顾新禹 GU, Xinyu; CN
薛佳 XUE, Jia; CN
谢玲玲 XIE, Lingling; 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:
201510618067.625.09.2015CN
Title (EN) PREPARATION METHOD OF COPANLISIB
(FR) PROCÉDÉ DE PRÉPARATION DE COPANLISIB
(ZH) 库潘尼西的制备方法
Abstract:
(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 (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)
Also published as:
KR1020180096572