METHOD OF SYNTHESIS OF 2-{4-[4-(4-CHLORO-1-PYRAZOLYL)BUTYL]-1-PIPERAZINYL}-PYRIMIDINE (LEZOPITRON) Russian patent published in 1998 - IPC

Abstract RU 2116305 C1

FIELD: organic chemistry and technology. SUBSTANCE: invention relates to the synthesis of lezopitron of the formula (I) by condensation of 2-(1-piperazinyl)-pyrimidine, 4-chloropyrazole and hydrocarbon derivative of the formula (III): X(CH2)4Y, where X and Y are similar or different and mean the group to be split off: iodine, bromine, chlorine, mesylhydroxy- and tosylhydroxy-group. Process is carried out at heating, preferably at 80-180 C, under pressure 1-5 atm in medium of aprotonic polar solvent in the presence of mineral or organic base, preferably alkaline metal carbonate. Dimethylformamide, dimethylsulfoxide, isopropanol, tert.-butanol, toluene and xylene can be used as a solvent. Reaction time is 1-24 h. Condensation is carried out preferably in the presence of one or some agents of phase transfer, for example, tetrabutyl ammonium salt. EFFECT: simplified method, improved purity and high yield of the end product. 7 cl

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RU 2 116 305 C1

Authors

Ramon Merse-Vidal'

Khordi Frigola-Konstansa

Dates

1998-07-27Published

1994-05-06Filed