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1. WO2022094668 - PROCESS FOR PREPARING HETEROCYCLIC METHANONE COMPOUNDS AND AZA-BICYCLO INTERMEDIATES THEREOF

Publication Number WO/2022/094668
Publication Date 12.05.2022
International Application No. PCT/AU2021/051310
International Filing Date 05.11.2021
IPC
C07D 451/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
04with hetero atoms directly attached in position 3 of the 8-azabicyclo octane or in position 7 of the 3-oxa-9-azatricyclo nonane ring system
06Oxygen atoms
A61K 31/506 2006.1
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 3/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 9/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
A61P 25/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
C07B 49/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
49Grignard reactions
Applicants
  • ACTINOGEN MEDICAL LIMITED [AU]/[AU]
Inventors
  • GRUGEL, Christian
Agents
  • FB RICE PTY LTD
Priority Data
202090406006.11.2020AU
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING HETEROCYCLIC METHANONE COMPOUNDS AND AZA-BICYCLO INTERMEDIATES THEREOF
(FR) PROCÉDÉ DE PRÉPARATION DE COMPOSÉS DE MÉTHANONE HÉTÉROCYCLIQUES ET DE LEURS INTERMÉDIAIRES AZA-BICYCLO
Abstract
(EN) The present disclosure relates to a process for synthesis of heterocyclic methanone compounds, and in particular 3'-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds, and aza-bicyclo intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of Xanamem. The present disclosure also relates to a process for the synthesis of optionally protected aza-bicyclo intermediate compounds. The present disclosure also relates to 3'-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and aza-bicyclo intermediate compounds thereof.
(FR) La présente divulgation concerne un procédé de synthèse de composés de méthanone hétérocycliques, et en particulier des composés 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophén-3-yl]-méthanone substitués en position 3' et leurs intermédiaires aza-bicyclo. En particulier, la présente divulgation concerne également un procédé de synthèse de Xanamem. La présente divulgation concerne également un procédé de synthèse de composés intermédiaires aza-bicyclo éventuellement protégés. La présente divulgation concerne également des composés 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophén-3-yl]-méthanone substitués en position 3' et leurs composés intermédiaires aza-bicyclo.
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