METHOD FOR PRODUCTION OF BENZHYDRYLOXYETHYLPIPERAZINE DERIVATIVES Russian patent published in 1995 - IPC

FIELD: organic chemistry, medicine. SUBSTANCE: desired products have formula I where R₁-H, Hal, lower alkyl, lower alkoxy, trifluormethyl; R₂-H, Hal, R₃-H, Hal, CF₃; n is integer 2-6, one of R₄ and R₅ being H, other being benzoyl which is substituted by NO₂ or CH₃O or R₄ и R₅ together with bound to them nitrogen atom forms heterocyclic group. Mentioned above heterocyclic group is represented by succinimidyl, 4-phenylsuccinimidyl, 2-oxobenzimidazolynyl, 3-benzyl-2-oxobenzimidazolynyl, 1,2,3,4-tetrahydro-2,4-dioxoquinazolynyl, 3,4-dihydro-4-oxoquinazolynyl, 3,4-dihydro-4-oxo2-methylqinazolynyl, 3,7-dihydro-1,3-dimethyl-2,6-dioxo- 1H-pyrinyl, 3,7-dihydro-3,7-dimethyl-2,6-dioxo-1H-pyrinyl. Amine having formula X-(CH₂)_n-NR₄R₅, where X is Hal, tosyl is used as reagent 1. Benzhydryloxyethylpiperazine is used as reagent 2. Reaction is carried out in aprotic solvent in excess of mentioned above amine. Proposed derivatives have antihistamine action. Mentioned above desired product have structural formula EFFECT: improved quality of desired product.