RS51855B - Microbiological method for the production of 7alpha- substituted 11 alpha-hydroxysteroids - Google Patents

Microbiological method for the production of 7alpha- substituted 11 alpha-hydroxysteroids

Info

Publication number
RS51855B
RS51855B YU20050045A YUP4505A RS51855B RS 51855 B RS51855 B RS 51855B YU 20050045 A YU20050045 A YU 20050045A YU P4505 A YUP4505 A YU P4505A RS 51855 B RS51855 B RS 51855B
Authority
RS
Serbia
Prior art keywords
substituted
stands
hydroxysteroids
7alpha
general formula
Prior art date
Application number
YU20050045A
Other languages
Serbian (sr)
Inventor
Rolf Bohlmann
Hermann Künzer
Reinhard Nubbemeyer
Hans-Peter Muhn
Ludwig Zorn
Norbert Gallus
Original Assignee
Bayer Schering Pharma Aktiengesellschaft
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE10233723A external-priority patent/DE10233723A1/en
Application filed by Bayer Schering Pharma Aktiengesellschaft filed Critical Bayer Schering Pharma Aktiengesellschaft
Publication of RS20050045A publication Critical patent/RS20050045A/en
Publication of RS51855B publication Critical patent/RS51855B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J11/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00—Preparation of steroids
    • C12P33/06—Hydroxylating
    • C12P33/08—Hydroxylating at 11 position
    • C12P33/10—Hydroxylating at 11 position at 11 alpha-position
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00—Preparation of steroids
    • C12P33/12—Acting on D ring
    • C12P33/16—Acting at 17 position

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Reproductive Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

MIKROBIOLOŠKI POSTUPAK ZA DOBIJANJE 7ALFA-SUPSTITUISANIH 11ALFA-HIDROKSISTEROIDA. Postupak za dobijanje 7α,17α-supstituisanih 11β-halogensteroida opšte fomiule 10,u kojoj jeR7 grupacija P-Q, pri čemuP predstavlja C1 do C4-alkilen a Q vodonik, C1 do C4-alkil ili C1- do C4-fluoroalkil a grupacija P-Q je vezana preko P za steroidni skelet,R10 stoji za H, CH3 ili CF3,R11 stoji za halogen,R13 stoji za metil ili etil,R17 stoji za CH3, C1- do C18-alkinil, CH2CN ili CF3, iR17 stoji za H,sa sledećim stupnjevima postupka:- Nukleofilna supstitucija na jednom 7a-supstituisanom 11α-hidroksisteroidu opšte formule 4,Bu kojojR7, R10 i R13 imaju gore pomenuto značenje,- u položaju 11 sa nekim halodehidroksilujućim reagensom;- reakcija tako nastalog 7α-supstituisanog 11β-halogensteroida sa nekim alkilujućim sredstvom selektivno na C17-atomu prstenastog skeleta u 7α,17α-supstituisani 11β-halogensteroid opšte formule 10.MICROBIOLOGICAL PROCEDURE FOR THE PREPARATION OF 7ALPHA-SUBSTITUTED 11ALPHA-HYDROXYSTEROIDS. A process for the preparation of 7α, 17α-substituted 11β-halidesteroids of general formula 10, wherein R7 is a PQ group, wherein P represents C1 to C4-alkylene and Q represents hydrogen, C1 to C4-alkyl or C1 to C4-fluoroalkyl and the PQ group is attached via P for steroid skeleton, R10 stands for H, CH3 or CF3, R11 stands for halogen, R13 stands for methyl or ethyl, R17 stands for CH3, C1- to C18-alkynyl, CH2CN or CF3, and R17 stands for H, with the following steps of the process: - Nucleophilic substitution on a 7α-substituted 11α-hydroxysteroid of general formula 4, Bu in which R7, R10 and R13 have the meaning mentioned above, by an alkylating agent selectively on the C17 atom of the ring skeleton in the 7α, 17α-substituted 11β-halogen steroid of general formula 10.

YU20050045A 2002-07-24 2003-07-24 Microbiological method for the production of 7alpha- substituted 11 alpha-hydroxysteroids RS51855B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10233723A DE10233723A1 (en) 2002-07-24 2002-07-24 Preparation of 7 alpha-substituted 11 alpha-hydroxy-steroids, useful as precursors for new androgenic 7 alpha,17 alpha-substituted 11 beta-halo-steroids, by microbiological conversion of 7 alpha-substituted steroids
US40295302P 2002-08-14 2002-08-14
PCT/EP2003/008111 WO2004011663A2 (en) 2002-07-24 2003-07-24 Microbiological method for the production of 7 alpha-substituted 11 alpha-hydroxysteroids

Publications (2)

Publication Number Publication Date
RS20050045A RS20050045A (en) 2007-06-04
RS51855B true RS51855B (en) 2012-02-29

Family

ID=31189296

Family Applications (1)

Application Number Title Priority Date Filing Date
YU20050045A RS51855B (en) 2002-07-24 2003-07-24 Microbiological method for the production of 7alpha- substituted 11 alpha-hydroxysteroids

Country Status (20)

Country Link
EP (1) EP1523568A2 (en)
JP (1) JP4417838B2 (en)
KR (1) KR101041328B1 (en)
CN (1) CN100339486C (en)
BR (1) BR0313210A (en)
CA (1) CA2492079C (en)
CO (1) CO5690563A2 (en)
CR (1) CR7672A (en)
EA (2) EA008147B1 (en)
EC (1) ECSP055630A (en)
HK (1) HK1081999A1 (en)
HR (1) HRP20050172A2 (en)
IL (1) IL166358A0 (en)
MX (1) MXPA05001024A (en)
NO (1) NO20050980L (en)
NZ (2) NZ537871A (en)
PH (1) PH12005500143B1 (en)
PL (1) PL373808A1 (en)
RS (1) RS51855B (en)
WO (1) WO2004011663A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1947107B1 (en) * 2005-10-27 2012-10-17 SRI International Process for production of steroid compound
CN103834712B (en) * 2012-11-26 2016-03-30 复旦大学 The optimization method of desogestrel intermediate nanometer liposome bio-transformation
CN103214543B (en) * 2012-12-25 2015-09-02 中国人民解放军海军医学研究所 New Crategolic acid derivative, its preparation method and the application in antitumor drug thereof
CN104862323B (en) * 2015-06-02 2018-01-16 中国农业科学院生物技术研究所 Modify the '-hydroxylase gene of diphenol compounds
PL442098A1 (en) * 2022-08-26 2024-03-04 Uniwersytet Przyrodniczy we Wrocławiu Method of producing 11α-hydroxy-19-nortestosterone

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE496261A (en) 1949-06-11
US2658023A (en) * 1953-04-21 1953-11-03 Pfizer & Co C Oxygenation of steroids
US2985563A (en) 1958-11-13 1961-05-23 Schering Corp 11alpha-hydroxylation of steroids by glomerella
US3004047A (en) 1959-03-13 1961-10-10 Olin Mathieson 6alpha-halo-11alpha-hydroxy steroids of the pregnane series and esters thereof
US3341557A (en) * 1961-06-05 1967-09-12 Upjohn Co 7-methyltestosterones
US3203869A (en) 1962-10-11 1965-08-31 Syntex Corp 11alpha-hydroxylation of 6-substituted-11-desoxy steroids with microorganisms of thegenus fusarium, liseola section
US5342834A (en) 1989-04-07 1994-08-30 The Population Council, Inc. Method for androgen supplementation
EP1167380A3 (en) 1995-12-11 2004-12-08 G.D. Searle & Co. 11.alpha.-hydroxy-steroid-4,6-dien-3-one compounds and a process for their preparation
PL185223B1 (en) * 1995-12-12 2003-04-30 Akzo Nobel Nv Microbiological method of 11alpha- hydroxylating the steroids
GB9525194D0 (en) 1995-12-12 1996-02-07 Zeneca Ltd Pharmaceutical composition
US6767902B2 (en) 1997-09-17 2004-07-27 The Population Council, Inc. Androgen as a male contraceptive and non-contraceptive androgen replacement
US20020012694A1 (en) * 1997-09-17 2002-01-31 Alfred J. Moo-Young Transdermal administration of ment
US5952319A (en) 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
EE200200454A (en) 2000-02-15 2003-12-15 Schering Aktiengesellschaft Male contraceptive containing norethisterone
DE10104327A1 (en) * 2001-01-24 2002-07-25 Schering Ag New 11beta-halo-testosterone derivatives useful in male hormone replacement therapy and in male fertility control
DE50308933D1 (en) * 2002-07-25 2008-02-14 Bayer Schering Pharma Ag COMPOSITION, CONTAINING AN ANDROGENIC 11-B HALOGEN STEROIDE AND A STATEMENT AND MALE CONTRAZEPTIVUM BASED ON THIS COMPOSITION

Also Published As

Publication number Publication date
CN1671858A (en) 2005-09-21
BR0313210A (en) 2005-06-28
CR7672A (en) 2006-05-29
MXPA05001024A (en) 2005-05-16
EP1523568A2 (en) 2005-04-20
PH12005500143B1 (en) 2011-03-25
CA2492079C (en) 2012-01-10
HK1081999A1 (en) 2006-05-26
NO20050980L (en) 2005-02-23
CO5690563A2 (en) 2006-10-31
NZ537871A (en) 2006-10-27
CA2492079A1 (en) 2004-02-05
WO2004011663A9 (en) 2004-05-06
WO2004011663A2 (en) 2004-02-05
WO2004011663A3 (en) 2004-07-15
KR20050026507A (en) 2005-03-15
EA200500224A1 (en) 2005-08-25
CN100339486C (en) 2007-09-26
IL166358A0 (en) 2006-01-16
EA200601030A1 (en) 2006-10-27
EA008147B1 (en) 2007-04-27
MX260952B (en) 2008-10-01
AU2003281677A1 (en) 2004-02-16
EA010572B1 (en) 2008-10-30
NZ549529A (en) 2008-04-30
RS20050045A (en) 2007-06-04
JP2006503813A (en) 2006-02-02
JP4417838B2 (en) 2010-02-17
PL373808A1 (en) 2005-09-19
HRP20050172A2 (en) 2005-04-30
KR101041328B1 (en) 2011-06-14
ECSP055630A (en) 2005-04-18

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