PROCESS FOR THE PREPARATION OF ARIPIPRAZOLE LAUROXIL

It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric acid in the presence of a suitable solvent and a carboxyl activating agent in the presence of a suitable solvent and, optionally, in the presence of an appropriate...

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Main Authors POMARES MARCO, Marta, MARQUILLAS OLONDRIZ, Francisco De Asís, BESSA BELLMUNT, Jorge, DE LEÓN MARTÍN, Antonio Abelino
Format Patent
LanguageEnglish
Published 07.05.2020
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric acid in the presence of a suitable solvent and a carboxyl activating agent in the presence of a suitable solvent and, optionally, in the presence of an appropriate base. -(Hydroxymethyl) aripiprazole can be prepared by reacting aripiprazole or an hydrate thereof with paraformaldehyde in the presence of a suitable organic 10 solvent and a suitable base, wherein the reaction is carried out without the addition of water as a solvent to the reaction mixture. Additionally, (7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-3,4-dihydro-2-oxoquinolin-1(2H)-yl)methyl formate is provided as a reference standard.
Bibliography:Application Number: US201816633757