METHOD OF ANDROSTANE-17 BETA-CARBOXYL ACID'S NEW ESTERS PRODUCTION

• Main Authors: AXELSSON BENGT I.,SE, THALEN BROR A.,SE, ANDERSSON PAUL H.,SE, ANDERSSON PER T.,SE, TROFAST JAN W.,SE
• Format: Patent
• Language: English
• Published: 14.04.1989
• Edition: 4
• 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

The invention refers to compounds having anti-inflammatory activity characterized by the formula or a stereoisomeric component thereof, in which formula X1 represents a hydrogen, chlorine, bromine or fluorine atom; X2 represents a hydrogen, chlorine, bromine or fluorine atom; R1 represents a beta -hydroxy group, a beta -chlorine atom or an oxo group; R2 represents a hydrogen atom, a methylene group or an alpha - or beta -methyl group; R3 represents a hydrogen atom or an acyl group of 1 through 8 carbon atoms; R4 represents a hydrogen atom, a (C1-C5) alkyl group or a phenyl group; R5 represents a hydrogen atom, a (C1-C5) alkyl group or a phenyl group; Y represents either CR7R8, O, S or NR9, where R7, R8 and R9 are selected from hydrogen or from straight or branched hydrocarbon chains having 1-8 carbon atoms or from a phenyl group. R6 represents a hydrogen; a methyl group; a phenyl or an alkenyl or cycloalkylene group optionally substituted by alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy and trifluoromethyl group(s); a (C1-C5) alkyl group substituted by at least one halogen atom; a saturated or unsaturated carbocyclic or heterocyclic (O, S, N) ring system containing 3-10 atoms in the ring system; a C1 alkyl group substituted by either one or two alicyclic or aromatic 3,4,5 or 6-numbered ring system(s) or one, two or three straight or branched alkyl or alkenyl group(s) of 1 through 18 carbon atoms; and represents a single or double bond. The invention also refers to a process and intermediates for the preparation of these compounds, a pharmaceutical preparation containing one of the compounds and a method for the treatment of inflammatory conditions.