DK160082A - METHOD FOR PREPARING 8- (4- (4- (2-PYRIMIDINYL) -1-PIPERAZINYL) -BUTYL) -8-AZAAPIRO (4,5) -DECAN-7,9-DION - Google Patents

METHOD FOR PREPARING 8- (4- (4- (2-PYRIMIDINYL) -1-PIPERAZINYL) -BUTYL) -8-AZAAPIRO (4,5) -DECAN-7,9-DION Download PDF

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Publication number
DK160082A
DK160082A DK160082A DK160082A DK160082A DK 160082 A DK160082 A DK 160082A DK 160082 A DK160082 A DK 160082A DK 160082 A DK160082 A DK 160082A DK 160082 A DK160082 A DK 160082A
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Prior art keywords
formula
image
compound
piperazinyl
pyrimidinyl
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DK160082A
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Danish (da)
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DK152730C (en
DK152730B (en
Inventor
P J Kairisalo
E J Honkanen
Original Assignee
Orion Yhtymae Oy
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Publication of DK160082A publication Critical patent/DK160082A/en
Publication of DK152730B publication Critical patent/DK152730B/en
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Publication of DK152730C publication Critical patent/DK152730C/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

The known compound 8-{4-[4-(2-pyrimidinyl)-1-piperazinyl]- butyl}-8-azaspiro(4,5)-decane-7,9-dione, buspiron, with formula <IMAGE>, I is prepared by reacting an 8-alkaline metal-8- azaspiro(4,5)-decane-7,9-dione with formula <IMAGE>, II with a 4-halogenbutylalkylsulphonate or -arylsulphonate with the formula <IMAGE>, III to form a compound with formula <IMAGE>, IV which is then reacted in known manner with a compound of formula <IMAGE>, V to form the desired product. One achieves high yield, around 90 per cent, by production of intermediate product IV, thereby making the method cheaper. The 4-halogenbutyl derivative can be prepared from 4- chloro-butanol and an appropriate sulphonic acid halide in presence of trimethylamine, and the reaction of this product with compound II advisedly occurs in N,N- diformamide at 80 degrees Celsius for two hours. Buspiron is a known pharmaceutical with sedative properties, among others.
DK160082A 1981-04-09 1982-04-07 METHOD FOR PREPARING 8-AE4-OE4- (2-PYRIMIDINYL) -1-PIPERAZINYLAA-BUTYLAA-8-AZASPIRO (4,5) -DECAN-7,9-DION DK152730C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI811108 1981-04-09
FI811108 1981-04-09

Publications (3)

Publication Number Publication Date
DK160082A true DK160082A (en) 1982-10-10
DK152730B DK152730B (en) 1988-05-02
DK152730C DK152730C (en) 1988-10-03

Family

ID=8514296

Family Applications (1)

Application Number Title Priority Date Filing Date
DK160082A DK152730C (en) 1981-04-09 1982-04-07 METHOD FOR PREPARING 8-AE4-OE4- (2-PYRIMIDINYL) -1-PIPERAZINYLAA-BUTYLAA-8-AZASPIRO (4,5) -DECAN-7,9-DION

Country Status (3)

Country Link
DK (1) DK152730C (en)
NO (1) NO821086L (en)
SE (1) SE449224B (en)

Also Published As

Publication number Publication date
SE8202132L (en) 1982-10-10
DK152730C (en) 1988-10-03
NO821086L (en) 1982-10-11
SE449224B (en) 1987-04-13
DK152730B (en) 1988-05-02

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