80486-69-7Relevant articles and documents
PROCESS FOR SYNTHESIS OF ANDROSTANE 17-BETA CARBOTHIOIC ACID AND RELATIVE COMPOUNDS THEREOF
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Page/Page column 4, (2009/12/02)
A process for synthesis of androstane 17-β carbothioic acid is provided. The process includes mixing an androstane 17-β carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-β carbothioic acid, wherein the androstane 17-β carbothioic acid has the formula (I): wherein R1 represents hydrogen or haloalkyl groups, R2 represents C1-8 linear alkyl groups, C1-8 branched alkyl groups, C1-6 unsaturated acyclic groups or aromatic groups, R3 represents hydrogen or hydroxyl, R4 represents hydrogen, bromine, chlorine or fluorine and R5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
ANDROSTANE CARBOTHIOATES
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, (2008/06/13)
Compounds of the formula wherein R1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R2 represents a group COR6 where R6 is a C 1-3 alkyl group or OR2 and R3 together form a 16alpha,17alpha-isopropylidenedioxy group; R3 represents a hydrogen atom, a methyl group (which may be in either the alpha- or beta -configuration) or a methylene group; R4 represents a hydrogen, chlorine or fluorine atom; R5 represents a hydrogen or fluorine atom and symbol represents a single or double bond have good anti-inflammatory activity, particularly on topical applications. The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9alpha-halo-11 beta-hydroxy grouping. Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed
