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1. WO2020204647 - PROCESSES FOR PREPARING (3R,4R)-1-BENZYL-N,4-DIMETHYLPIPERIDIN-3-AMINE OR A SALT THEREOF AND PROCESSES FOR PREPARING TOFACITINIB USING THE SAME

Publication Number WO/2020/204647
Publication Date 08.10.2020
International Application No. PCT/KR2020/004547
International Filing Date 03.04.2020
IPC
C07D 211/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with 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
56Nitrogen atoms
C07D 211/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
02Preparation by ring-closure or hydrogenation
A61K 31/4418 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4418having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61P 1/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 19/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants
  • YUHAN CORPORATION [KR]/[KR]
Inventors
  • OH, Sang-Ho
  • LEE, Doo-Byung
  • KWON, Kyoung-Chan
  • KIM, Sang-Won
  • HWANG, Hyo-Ick
  • LEE, Kyeong-Sill
  • JO, Ik-Su
  • CHOI, Ji-Hye
  • CHO, Sung-Hee
  • LEE, Su-Young
Agents
  • OH, Kook-Jin
Priority Data
10-2019-004038305.04.2019KR
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES FOR PREPARING (3R,4R)-1-BENZYL-N,4-DIMETHYLPIPERIDIN-3-AMINE OR A SALT THEREOF AND PROCESSES FOR PREPARING TOFACITINIB USING THE SAME
(FR) PROCÉDÉS DE PRÉPARATION DE (3R,4R)-1-BENZYL-N,4-DIMÉTHYLPIPÉRIDIN-3-AMINE OU D'UN SEL DE CELUI-CI ET PROCÉDÉS DE PRÉPARATION DE TOFACITINIB L'UTILISANT
Abstract
(EN)
The present invention provides a novel process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib. The present invention also provides a novel intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate. The present invention also provides a novel intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate. In addition, the present invention provides a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof using the process.
(FR)
La présente invention concerne un nouveau procédé de préparation de (3R,4R)-1-benzyl-N,4-diméthylpipéridin-3-amine ou d'un sel de celui-ci, qui est un intermédiaire utile pour la préparation de tofacitinib. La présente invention concerne également un nouvel intermédiaire utilisé dans le procédé, à savoir, un solvate d'isopropanol de ((3R,4R)-1-benzyl-4-méthylpipéridin-3-yl)carbamate dibenzoyl-L-tartrate de méthyle. La présente invention concerne en outre un nouvel intermédiaire, ayant une excellente stabilité, utile pour la préparation de tofacitinib, c'est-à-dire, l'acétate de (3R,4R)-1-benzyl-N,4-diméthylpipéridin-3-amine. De plus, la présente invention concerne un procédé de préparation de tofacitinib ou d'un sel pharmaceutiquement acceptable de celui-ci à l'aide du procédé.
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