PROCESS FOR THE PREPARATION OF BERAPROST OR SIMILAR BENZOPROSTACYCLIN ANALOGUES STARTING FROM 2-(3-BROMO-2-FLUOROPHENYL)-4-HYDROXYCYCLOPENT-2-ENONE OR SIMILAR REACTANTS

The present invention relates to a process for preparing benzoprostacyclin analogues such as e.g. beraprost (4-((1 RS ,2 RS ,3a SR ,8b SR )-2-hydroxy-1-((3 SR , E )-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2,3,3a,8b-tetrahydro-1 H -cyclopenta[ b ]benzofuran-5-yl)butanoic acid)starting from cyclopenteno...

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Bibliographic Details
Main Authors LIN, Chun-Yu, WEI, Tzyh-Mann, WEI, Shih-Yi
Format Patent
LanguageEnglish
French
German
Published 07.12.2022
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to a process for preparing benzoprostacyclin analogues such as e.g. beraprost (4-((1 RS ,2 RS ,3a SR ,8b SR )-2-hydroxy-1-((3 SR , E )-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2,3,3a,8b-tetrahydro-1 H -cyclopenta[ b ]benzofuran-5-yl)butanoic acid)starting from cyclopentenone intermediates e.g. of formula I in racemic or optically enriched formsuch as e.g. 2-(3-bromo-2-fluorophenyl)-4-hydroxycyclopent-2-enoneBeraprost and its enantiomerically pure beraprost-314d stereoisomer are pharmacologically active compounds for the treatment of pulmonary hypertension and vascular diseases.
Bibliography:Application Number: EP20220172492