2-4-[4-(4,5-DICHLORO-2-METHYLIMIDAZOLE-1-YL)BUTYL]-1-PIPERAZINYL-5-FLUOROPYRIMIDINE, ITS SYNTHESIS AND THERAPEUTIC USING Russian patent published in 2002 - IPC

Abstract RU 2191184 C2

FIELD: organic chemistry of heterocyclic compounds, medicine, pharmacy. SUBSTANCE: invention relates to a novel 2-4-[4-(4,5-dichloro-2-methylimidazole-1-yl)butyl] -1-piperazinyl-5-fluoropyrimidine of the formula (I) and to its physiologically acceptable salts, for example, citrate, methods of their synthesis and a pharmaceutical composition. The compound of the formula (I) is synthesized by reaction of 8-(5-fluoro-2-pyrimidinyl)-8- aza-5-azoniaspiro-[4,5]-decane with 4-dichloro-2-methyl-1H-imidazole in the presence of potassium carbonate in medium of a polar solvent, for example, dimethylformamide at a boiling point of reaction from 70 C to a solvent boiling point for 3-48 h; or by reaction of 5-fluoro-2-(piperazine-1-yl)-pyrimidine with 1-(4-chlorobutyl-4,5-dichloro- 2-methyl-1H-imidazole under the above indicated conditions or under conditions of the phase transition using an aqueous solution of sodium hydroxide, toluene and a catalyst, for example, tetrabutylammonium bromide at temperature from 50 C to 90 C for from 12 to 72 h. The proposed pharmaceutical composition comprises a compound of the formula (I), its physiologically acceptable salts and a pharmaceutically acceptable base. Compounds of the formula (I) can be used for preparing a medicinal agent designated for treatment of vertigo, transport sick (nausea), depression, troubling state, acid secretion in stomach, obsessive or compulsive disorders, panic attacks and apnea during sleep. EFFECT: new compound indicated above, improved method of synthesis, valuable medicinal properties. 7 cl, 6 ex

Similar patents RU2191184C2

Title Year Author Number
DERIVATIVES OF 2-[4-(4-AZOLYLBUTYL)-1-PIPERAZINYL]-PYRIMIDINE OR THEIR PHYSIOLOGICALLY ACCEPTABLE SALTS, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1994
  • Khordi Frigola Konstansa
  • Ramon Merse-Vidal'
RU2118318C1
METHOD OF SYNTHESIS OF DERIVATIVES OF ARYL- OR HETEROARYLPIPERAZINYLBUTYLAZOLE 1992
  • Ramon Merse Vidal'[Es]
  • Zhordi Frigalo Konstansa[Es]
  • Zhuan Pares Korominas[Es]
RU2053230C1
DERIVATIVES OF ARYL- (OR HETEROARYL)-PIPERAZINYLALKYLAZOLES, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1992
  • Ramon Merse Vidal'[Es]
  • Khordi Frigola Konstansa[Es]
  • Khuan Pares Korominas[Es]
RU2088582C1
TETRAHYDROPYRIDINE- OR 4-HYDROXYPIPERIDINEALKYLAZOLES OR THEIR PHYSIOLOGICALLY ACCEPTABLE SALTS, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1995
  • Ramon Merse-Vidal
  • Khordi Frigola-Konstantsa
RU2168507C2
BENZIMIDAZOLE DERIVATIVES SHOWING ANTIHISTAMINE ACTIVITY 1991
  • Marija Rosa Kuberes-Al'Tisent[Es]
  • Khordi Frigola-Konstansa[Es]
  • Khuan Pares-Korominas[Es]
RU2024519C1
APPLICATION OF DERIVATIVES OF TETRAHYDROPYRIDINE (OR 4-HYDROXYPIPERIDINE)BUTYLAZOLES AS ANALGETICS 1999
  • Merse-Vidal' Ramon
  • Frigola-Konstansa Khordi
RU2202347C2
AGENT FOR COGNITIVE FUNCTION IMPROVEMENT 1992
  • Khordi Frigola-Konstansa[Es]
  • Khuan Pares-Korominas[Es]
RU2078568C1
METHOD OF SYNTHESIS OF 2-{4-[4-(4-CHLORO-1-PYRAZOLYL)BUTYL]-1-PIPERAZINYL}-PYRIMIDINE (LEZOPITRON) 1994
  • Ramon Merse-Vidal'
  • Khordi Frigola-Konstansa
RU2116305C1
DERIVATIVES OF 4-(2-PYRIMIDINYL)-1-PIPERAZINYL OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 1991
  • Ogusto Kolombo Pinol'[Es]
  • Khordi Frigola Konstansa[Es]
  • Khuan Pares Korominas[Es]
RU2071474C1
NOVEL POLYMORPHOUS FORMS OF LESOPITRON DIHYDROCHLORIDE AND HYDRATE FORMS THEREOF, PREPARATION METHODS, AND COMPOSITIONS BASED ON THEM 1996
  • Pilar Lupon Roses
  • Khajme Tomas Navarro
  • Sal'Vador Puig Torres
  • Khordi Frigola Konstansa
RU2178789C2

RU 2 191 184 C2

Authors

Merse-Vidal' Ramon

Frigola-Konstansa Khordi

Dates

2002-10-20Published

1998-05-28Filed