Related Experiment Video
Updated: Jun 14, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Optimization of aripiprazole synthesis
Andrzej Leś1, Katarzyna Badowska-Rosłonek, Marta Łaszcz
1Pharmaceutical Research Institute, Rydygiera 8, 01-793 Warszawa, Poland. a.les@ifarm.waw.pl
Abstract:
A series of aripiprazole (AR3) syntheses were performed at laboratory scale (10 mmol of the ARI substrate) in order to optimize the amount of another substrate AR2, as well as Na2CO3, ethanol and varying the reaction time. The reaction parameters were chosen according to the D-optimal plans. A high conversion ratio, about 90-99%, was obtained. Purity of crude product (AR3) was determined by HPLC. Molar content of crude reaction product was predicted theoretically with the use of the mass balance and the corresponding HPLC parameters. The theoretical predictions were verified with the potentiometric and thermogravimetric analysis of selected samples. Based on the predicted molar content of reaction mixtures, a series of reaction response surfaces was calculated and optimal set of reaction parameters for aripiprazole synthesis was determined.
Related Concept Videos
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Preparation of 1° Amines: Gabriel Synthesis
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview

