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1. (WO2019026004) PROCESS FOR PREPARING 1 -(((Z)-(1 -(2-AMINOTHIAZOL-4-YL)-2-OXO-2-(((3S,4R)-2-OXO-4-((2-OXOOXAZOLIDIN-3-Y L)METHYL)-1 -SULFOAZETIDIN-3- YL)AMINO)ETHYLIDENE)AMINO)OXY)CYCLOPROPANE CARBOXYLIC ACID
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Pub. No.: WO/2019/026004 International Application No.: PCT/IB2018/055789
Publication Date: 07.02.2019 International Filing Date: 01.08.2018
IPC:
C07D 417/14 (2006.01) ,C07D 263/24 (2006.01) ,C07D 413/06 (2006.01) ,C07C 13/04 (2006.01) ,C07C 229/48 (2006.01) ,C07C 291/04 (2006.01) ,A61K 31/427 (2006.01) ,A61P 31/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
08
having one double bond between ring members or between a ring member and a non-ring member
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
Oxygen atoms
20
attached in position 2
24
with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
13
Cyclic hydrocarbons containing rings other than, or in addition to, six-membered aromatic rings
02
Monocyclic hydrocarbons or acyclic hydrocarbon derivatives thereof
04
with a three-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
46
having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
48
with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
291
Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/-C07C281/144
02
containing nitrogen-oxide bonds
04
containing amino-oxide bonds
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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
Applicants:
NOVARTIS AG [CH/CH]; Lichtstrasse 35 4056 Basel, CH
Inventors:
CHEN, Like; CN
CHEUNG, Chi Ming; CN
FEI, Zhongbo; CN
JIANG, Qun; CN
LEI, Li; CN
LI, Bin; CN
RUCH, Thomas; CH
WANG, Hao; CN
WU, Quanbing; CN
Agent:
WEISS, Wolfgang; Weickmann & Weickmann Patentanwälte-Rechtsanwalt PartmbB Richard-Strauss-Straße 80 81679 München, DE
Priority Data:
PCT/CN2017/09561702.08.2017CN
Title (EN) PROCESS FOR PREPARING 1 -(((Z)-(1 -(2-AMINOTHIAZOL-4-YL)-2-OXO-2-(((3S,4R)-2-OXO-4-((2-OXOOXAZOLIDIN-3-Y L)METHYL)-1 -SULFOAZETIDIN-3- YL)AMINO)ETHYLIDENE)AMINO)OXY)CYCLOPROPANE CARBOXYLIC ACID
(FR) PROCESSUS CHIMIQUE DE PRÉPARATION D'ANTIBIOTIQUE MONOBACTAME ET DE SES INTERMÉDIAIRES
Abstract:
(EN) The present invention provides a process of synthesizing 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (referred to herein as Compound X), or a salt thereof, or a solvate including hydrate thereof, and/or intermediates thereof, and the use of intermediates for preparing Compound X. In particular, the process relates to the preparation of Compound X using dynamic kinetic resolution (DKR) and asymmetric catalytic reduction, thereby providing an improved route to 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (Compound X) and compositions containing said compound, including the arginine salt, sodium salt and hydrated solid forms of Compound X.
(FR) La présente invention concerne un processus de synthèse d'acide 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)méthyl)-1-sulfoazétidin-3 yl)amino)éthylidène)amino)oxy)cyclopropane carboxylique (appelé ici composé X), ou un sel de celui-ci, ou un solvate comprenant un hydrate de celui-ci, et/ou des intermédiaires de celui-ci, et l'utilisation d'intermédiaires pour préparer le composé X. En particulier, le processus concerne la préparation du composé X à l'aide d'une résolution cinétique dynamique (DKR) et d'une réduction catalytique asymétrique, ce qui permet d'obtenir une route améliorée vers l'acide 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)méthyl)-1-sulfoazétidin-3 yl)amino)éthylidène)amino)oxy)cyclopropane carboxylique (composé X) et des compositions contenant ledit composé, y compris le sel d'arginine, le sel de sodium et les formes solides hydratées du composé X.
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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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: English (EN)
Filing Language: English (EN)