GB1013229A - A process for the manufacture of benzodiazepine derivatives - Google Patents

A process for the manufacture of benzodiazepine derivatives

Info

Publication number
GB1013229A
GB1013229A GB909463A GB909463A GB1013229A GB 1013229 A GB1013229 A GB 1013229A GB 909463 A GB909463 A GB 909463A GB 909463 A GB909463 A GB 909463A GB 1013229 A GB1013229 A GB 1013229A
Authority
GB
United Kingdom
Prior art keywords
group
alkyl
halogen atom
pharmaceutical preparations
acid addition
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
GB909463A
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 US240750A external-priority patent/US3340253A/en
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of GB1013229A publication Critical patent/GB1013229A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20—Nitrogen atoms
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C07D243/26—Preparation from compounds already containing the benzodiazepine skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Inductance-Capacitance Distribution Constants And Capacitance-Resistance Oscillators (AREA)

Abstract

The invention comprises compounds of the general formula <FORM:1013229/C2/1> (wherein R1 represents an alkanoyl, aralkanoyl, aroyl or alkyl group, R2 represents a halogen atom or trifluoromethyl group, R3 represents a halogen atom or an alkyl, alkylthio, nitro or trifluoromethyl group, R4 represents an alkyl or alkenyl group, and the broken lines denote optional substituents) and acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by subjecting a compound of the formula <FORM:1013229/C2/2> to acylation with an aliphatic, araliphatic or aromatic carboxylic acid anhydride, sulphide or halide, optionally followed by (a) one or both of the steps of hydrolysis and reaction with an alkanol (consecutively or simultaneously when both steps are required), (b) introduction of the R4 group at any stage when not present in the starting material, and/or (c) acid addition salt formation at any suitable stage. The compounds of the invention are sedatives, anticonvulsants and muscle relaxants, and may be administered enterally or parenterally in the form of pharmaceutical preparations (e.g. tablets, dragees, suppositories, capsules, solutions, emulsions and suspensions) containing them, with or without other (unspecified) active ingredients, in association with a carrier. Specification 972,968 is referred to.
GB909463A 1962-03-09 1963-03-07 A process for the manufacture of benzodiazepine derivatives Expired GB1013229A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17855162A 1962-03-09 1962-03-09
US240750A US3340253A (en) 1962-11-28 1962-11-28 Preparation of certain benzodiazepine compounds

Publications (1)

Publication Number Publication Date
GB1013229A true GB1013229A (en) 1965-12-15

Family

ID=26874429

Family Applications (2)

Application Number Title Priority Date Filing Date
GB4791264A Expired GB1013900A (en) 1962-03-09 1963-03-07 1,4-benzodiazepine derivatives and a process for the manufacture thereof
GB909463A Expired GB1013229A (en) 1962-03-09 1963-03-07 A process for the manufacture of benzodiazepine derivatives

Family Applications Before (1)

Application Number Title Priority Date Filing Date
GB4791264A Expired GB1013900A (en) 1962-03-09 1963-03-07 1,4-benzodiazepine derivatives and a process for the manufacture thereof

Country Status (9)

Country Link
BE (1) BE629227A (en)
CA (1) CA976547A (en)
CH (2) CH442326A (en)
DE (4) DE1545957A1 (en)
DK (1) DK127507B (en)
ES (1) ES285854A1 (en)
GB (2) GB1013900A (en)
NL (3) NL7010712A (en)
SE (2) SE328583B (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES405260A1 (en) * 1972-07-28 1975-07-01 Stabilimenti Chim Farmac Riuni Benzodiazepine compounds for therepeutical use
FR2269349B1 (en) * 1974-04-30 1979-03-16 Ferrer Labor
DE3413592C2 (en) * 1984-04-11 1986-06-05 Dolorgiet GmbH & Co KG, 5205 St Augustin Medicaments containing 5- (2-fluorophenyl) -1,3-dihydro-3-hydroxy-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one
ES8609278A1 (en) * 1984-06-26 1986-09-01 Merck & Co Inc Benzodiazepine derivatives and pharmaceutical compositions containing them.

Also Published As

Publication number Publication date
NL7010712A (en) 1970-10-26
NL289735A (en)
CA976547A (en) 1975-10-21
DE1445873A1 (en) 1969-04-10
GB1013900A (en) 1965-12-22
SE328583B (en) 1970-09-21
CH442326A (en) 1967-08-31
DE1545957A1 (en) 1969-12-11
ES285854A1 (en) 1963-08-16
DK127507B (en) 1973-11-19
SE361174B (en) 1973-10-22
CH457464A (en) 1968-06-15
DE1545956A1 (en) 1969-11-20
BE629227A (en) 1963-10-21
NL7010711A (en) 1970-10-26
DE1545955A1 (en) 1969-11-20

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