Method for manufacture of sertindole
AssigneeH. Lundbeck A/S
InventorsJacopo Zanon, Marco Villa, Francesco Ciardella
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Abstract
The present invention relates to a novel method for manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole wherein the method for manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide in the presence of a base, a chelating ligand and catalytic amounts or a copper salt comprising copper(I) or copper(II) and an anion which does not interfere in an unfavourable way with the reaction.
Claims20
A method for the manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole, wherein the manufacturing of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide, in a solvent of toluene or mixtures of toluene and water, in the presence of a base, a chelating ligand and a catalytic amount of a copper salt comprising copper(I) or copper(II), and an anion selected from the group consisting of (Cl−), (Br−), (I−), (OCOCH3), (SO4−), (CO3−2), and (O−4).
A method for the manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprising reacting 5-chloro-indole with a 4-fluorophenylhalide, in a solvent of toluene or mixtures of toluene and water, in the presence of a base, a chelating ligand and a catalytic amount of a copper salt comprising copper(I) or copper(II), and an anion selected from the group consisting of (Cl−), (Br−), (I−), (OCOCH3), (SO4−), (CO3−2), and (O−4).
Dependencies are inferred from the claim text.