PHOSPHORYLIZED DERIVATIVES OF 4-{4-[4-(HYDROXY-DIPHENYL)-1-PIPERIDINYL]-1-HYDROXY-BUTYL}-ALPHA-ALPHA-DIMETHYL-PHENYL-ACETIC ACID AND PROCESS FOR PRODUCING THEM

• Main Authors: WORM, MANFRED DR, MEIWES, JOHANNES DR
• Format: Patent
• Language: English; Hungarian
• Published: 28.12.2005
• Edition: 7
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; BEER; BIOCHEMISTRY; CHEMISTRY; ENZYMOLOGY; FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES USING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

Preparation of piperidine derivatives of formula (II) comprises incubating alpha -(p-tert.-butylphenyl)-4-( alpha -hydroxy- alpha -phenylbenzyl)-1-piperidine butanol or optionally 4-(4-(4-hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)- alpha , alpha -dimethylacetic acid with a Cunninghamella or Absidia fungus. R1 = OH or CH2-O-P(O)(OH)2; and R2 = OH; or R1 = CH3; and R2 = -O-P(O)(OH)2; or R2 = -O-P(O)(OH)2; and R1 = COOH. Also claimed are: (i) (II) except that R1 is not OH when R2 is OH; and (ii) preparation of a piperazine derivative of formula (I) comprising incubating alpha -(p-tert.-butylphenyl)-4-( alpha -hydroxy- alpha -phenylbenzyl)-1-piperidine butanol with a Cunninghamella or Absidia fungus.