Process for the esterification of a carbothioic acid

Disclosed is a process for preparing compounds of formula: (II) by esterification of the C-17 hydroxyl group of 6alpha, 9alpha-difluoro-11beta, 17alpha-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carbothioic acid. The process comprises treating compound (I) with a slight excess of an acy...

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Bibliographic Details
Main Authors HEGGIE, WILLIAM, SOBRAL, LUIS, MARTIN, DIONISIO, LEITAO, EMILLIA
Format Patent
LanguageEnglish
Published 31.03.2009
Edition7
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Summary:Disclosed is a process for preparing compounds of formula: (II) by esterification of the C-17 hydroxyl group of 6alpha, 9alpha-difluoro-11beta, 17alpha-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carbothioic acid. The process comprises treating compound (I) with a slight excess of an acyl chloride of general formula R-COCI, where R represents -CH2CH3, -CH2CH2CH3 or -CH(CH3)2, in an inert solvent, in the presence of a tertiary amine. Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5°C to -20 °C.
Bibliography:Application Number: NZ20040554865