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1. (WO2017096996) PREPARATION METHOD FOR COBIMETINIB
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/096996 International Application No.: PCT/CN2016/098853
Publication Date: 15.06.2017 International Filing Date: 13.09.2016
IPC:
C07D 401/04 (2006.01) ,A61K 31/397 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
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
397
having four-membered rings, e.g. azetidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
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:
201510906811.209.12.2015CN
Title (EN) PREPARATION METHOD FOR COBIMETINIB
(FR) PROCÉDÉ DE PRÉPARATION DE COBIMETINIB
(ZH) 卡比替尼的制备方法
Abstract:
(EN) A preparation method for cobimetinib (XL518, GDC-0973) (I). Preparation steps comprise: (2S)-2-piperidinecarboxylic acid, serving as a raw material, undergoes nitrification, hydrolysis, esterification, and Boc protection to produce an intermediate, [2-oxo-2-((2S)-1-tert-butoxycarbonylpiperidin-2-yl)] acetate, the intermediate underdoes an addition reaction, a reduction reaction, and a cyclization reaction to produce an intermediate, (2S)-1-tert-butoxycarbonyl-2-(3-hydroxyazetidin-3-yl) piperidine, followed by a condensation reaction with a side chain to produce cobimetinib (I). The preparation method has readily available raw materials and a simple process and is economical, environmentally friendly, and suitable for industrialized production.
(FR) L'invention concerne un procédé de préparation de cobimetinib (XL518, GDC-0973) (I). Les étapes de préparation consistent en les opérations suivantes : de l'acide (2S)-2-pipéridinecarboxylique, faisant office de matière première, subit une nitrification, une hydrolyse, une estérification, et une protection Boc pour produire un intermédiaire, de l'acétate [2-oxo-2-((2S)-1-tert-butoxycarbonylpiperidin-2-yle)], l'intermédiaire subit une réaction d'addition, une réaction de réduction, et une réaction de cyclisation pour produire un intermédiaire, de la pipéridine (2S)-1-tert-butoxycarbonyl-2-(3-hydroxyazétidin-3-yle), puis on provoque une réaction de condensation avec une chaîne latérale pour produire le cobimetinib (I). Le procédé de préparation fait appel à des matières premières faciles à obtenir et à un processus simple, il est économique et respectueux de l'environnement, et est approprié pour une production à l'échelle industrielle.
(ZH) 一种卡比替尼(Cobimetinib,XL518,GDC-0973)(I)的制备方法,其制备步骤包括:以(2S)-2-哌啶甲酸为原料,经酰腈化、水解、酯化和Boc保护制得中间体[2-氧代-2-((2S)-1-叔丁氧羰基哌啶-2-基)]乙酸酯,该中间体经加成反应、还原反应和环合反应制得中间体(2S)-1-叔丁氧羰基-2-(3-羟基氮杂环丁烷-3-基)哌啶,继而与侧链发生缩合反应制得卡比替尼(I),该制备方法原料易得,工艺简洁,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, KW, 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)