Process for the preparation of S-fluoromethyl-6,9-difluoro-11-hydroxy-16-methyl-17-propionyloxy-3-oxo-androsta-1,4-diene-17-carbothioate and intermediates

Process for the preparation of S-fluoromethyl-6,9-difluoro-11-hydroxy-16-methyl-17-propionyloxy-3-oxo-androsta-1,4-diene-17-carbothioate and intermediates

The present invention relates to a process for the preparation of steroidal 17²-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17²-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introd...

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Hauptverfasser: GADAKAR, Maheshkumar, Gore, Vinayak G, POKHARKAR, K, WAKCHAURE, Vikas
Format: Patent
Sprache:eng ; fre ; ger
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CHEMISTRY
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
STEROIDS
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creator GADAKAR, Maheshkumar
Gore, Vinayak G
POKHARKAR, K
WAKCHAURE, Vikas
description The present invention relates to a process for the preparation of steroidal 17²-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17²-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.
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subjects CHEMISTRY
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
STEROIDS
title Process for the preparation of S-fluoromethyl-6,9-difluoro-11-hydroxy-16-methyl-17-propionyloxy-3-oxo-androsta-1,4-diene-17-carbothioate and intermediates
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