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GB1026501A - Improvements in or relating to steroids and the manufacture thereof - Google Patents

Improvements in or relating to steroids and the manufacture thereof

Info

Publication number
GB1026501A
GB1026501A GB38760/62A GB3876062A GB1026501A GB 1026501 A GB1026501 A GB 1026501A GB 38760/62 A GB38760/62 A GB 38760/62A GB 3876062 A GB3876062 A GB 3876062A GB 1026501 A GB1026501 A GB 1026501A
Authority
GB
United Kingdom
Prior art keywords
chloro
dione
pregnadiene
acylate
trihydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
GB38760/62A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmacia and Upjohn Co
Original Assignee
Upjohn Co
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 US144830A external-priority patent/US3137712A/en
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of GB1026501A publication Critical patent/GB1026501A/en
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J75/00Processes for the preparation of steroids in general

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention comprises 16a -chloro steriods of the structural formula <FORM:1026501/C2/1> wherein R is hydroxyl, OAcyl or -OPO3H, the term Acyl representing the acyl radical of a hydrocarbon carboxylic acid containing from 1-12 carbon atoms, inclusive, R1 is an alkyl or aryl organic sulphonyl radical, X is hydrogen or fluorine, X1 is bromine or chlorine, Y is hydrogen, methyl or fluorine and processes for the preparation thereof by oxidatively hydroxylating an 11b -hydroxy-16a -chloro-21-acyloxy-1,4,17 (20-pregnatriene-3-one to produce 11b , 17a ,21-trihydroxy-16a -chloro-1,4-pregnadiene-3,20-dione 21-acylate III, dehydrating III with an N-haloacylamide and sulphur dioxide to form a 17a ,21-dihydroxy-16a -chloro-1,4,9(11)-pregnatriene-3,20 -dione 21-acylate IV, treating IV with an N-haloacylamide to form the corresponding 11b ,17a ,21 - trihydroxy - 9a - chloro-, bromo- or iodo-16a -chloro-1,4-pregnadiene-3,20-dione 21-acylate V; treating V with a mild base such as sodium acetate to form a 9b ,11b -oxido-17a ,21 -dihydroxy-16a -chloro-1,4-pregnadiene-3,20-dione 21-acylate VI, and treating VI with HF to form a 9a -fluoro-11b ,17a ,21-trihydroxy-16a - chloro - 1,4 - pregnadiene - 3,20 - dione 21-acylate. The oxidative hydroxylation may be effected with osmium tetroxide and an organic peroxide or an aryliodoso acetate. The 21-hydroxy compounds so obtained may be converted into the corresponding 21-sulphonyloxy compounds by means of an organic sulphonyl halide, which on further treatment with sodium or potassium iodide yield the corresponding 21-iodo compound. The 21-iodo compounds on treatment with silver dihydrogen phosphate gives 16a - chloro - 11b ,17a ,21 - trihydroxy - 1,4- pregnadiene - 3,20 - dione - 21 - dihydrogen phosphate which may be esterified in 17-position, or with silver fluoride 16a -chloro-21-fluoro-11b , 17a -dihydroxy-1,4-pregnadiene-3,20-dione is obtained.ALSO:Pharmaceutical compositions having anti-inflammatory and glucocorticoid activity and containing compounds having the formula <FORM:1026501/A5-A6/1> (wherein R is hydroxyl, O Acyl or OPO3H2, the term acyl representing the acyl radical of an organic carboxylic acid having 1-12 carbon atoms inclusive; X is hydrogen or fluorine and Y is hydrogen methyl or fluorine) are administered orally in pills, tablets, capsules, syrups elixirs, powders and granules, parenterally in sterile liquid form or topically in the forms of ointments, creams and lotions with or without coacting antibiotics e.g. chloramphenicol, penicillin, tetracyclines, erythromycin, novobiocin, polymyxin and bacitracin; analgesics e.g. aspirin, sodium salicylate, N-acetyl-p-aminophenol and salicylamide; amphetamines and tranquillizers; local anesthetics e.g. benzocaine, procaine and tetracaine; antacids, such as calcium carbonate, aluminium hydroxide, basic aluminium carbonate and bismuth subcarbonate; and the vitamins e.g. ascorbic acid and the Vitamin B-complex. The tablets can be laminated to form an inner-dosage and an outer-dosage component separated by an enteric layer thereby obtaining a delayed release. Alternatively the two components system can be utilized for preparing tablets containing incompatible ingredients.
GB38760/62A 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof Expired GB1026501A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US144830A US3137712A (en) 1961-10-13 1961-10-13 16alpha-chloro-1, 4-pregnadienes
US20240362A 1962-06-14 1962-06-14

Publications (1)

Publication Number Publication Date
GB1026501A true GB1026501A (en) 1966-04-20

Family

ID=26842402

Family Applications (3)

Application Number Title Priority Date Filing Date
GB38760/62A Expired GB1026501A (en) 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof
GB49713/65A Expired GB1026503A (en) 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof
GB49712/65A Expired GB1026502A (en) 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof

Family Applications After (2)

Application Number Title Priority Date Filing Date
GB49713/65A Expired GB1026503A (en) 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof
GB49712/65A Expired GB1026502A (en) 1961-10-13 1962-10-12 Improvements in or relating to steroids and the manufacture thereof

Country Status (2)

Country Link
FR (1) FR2260M (en)
GB (3) GB1026501A (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19715594A1 (en) 1997-04-15 1998-10-22 Bayer Ag Analgesic combination

Also Published As

Publication number Publication date
FR2260M (en) 1964-01-06
GB1026503A (en) 1966-04-20
GB1026502A (en) 1966-04-20

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