Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: Identification of a novel atypical neuroleptic

…, P DeBoer, E Meier, H Wikström

Index: Liao, Yi; DeBoer, Peter; Meier, Eddie; Wikstroem, Hakan Journal of Medicinal Chemistry, 1997 , vol. 40, # 25 p. 4146 - 4153

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Citation Number: 15

Abstract

The trifluoromethanesulfonyloxy (TfO) analogues 3 and 4 of 8-chloro-11-(4-methyl-1- piperazinyl)-5 H-dibenzo [b, e][1, 4] diazepine (clozapine, 1) and its 2-chloro isomer (iso- clozapine, 2), respectively, were synthesized via their OMe and OH analogues with the conventional synthetic method of the tricyclic dibenzodiazepines and evaluated pharmacologically along with their parent drugs. The binding profile of the 2-OTf analogue ...