Related Experiment Video
Updated: Jul 5, 2025

Optimized Griess Reaction for UV-Vis and Naked-eye Determination of Anti-malarial Primaquine
Published on: October 11, 2019
Process Development for the Manufacture of the Antimalarial Amodiaquine Dihydrochloride Dihydrate
Mukut Gohain1, Modibo S Malefo1, Phaladi Kunyane1
1Department of Research and Development at Chemical Process Technologies (Pty) Ltd, 45 Battery Crescent, Waltloo, City of Tshwane, Gauteng 0184, South Africa.
Abstract:
A robust process for the manufacture of the active pharmaceutical ingredient (API) amodiaquine dihydrochloride dihydrate (ADQ, 3), an important antimalarial, is reported. The process consists of a three-step synthetic route that involves a Mannich reaction, substitution with 4,7-dichloroquinoline (4,7-DCQ, 5), and rehydration. Additionally, a cost-competitive process for the production of 4,7-DCQ (5) is also reported wherein 4,7-DCQ (5) was prepared in four steps from meta-chloroaniline (7). 4-Acetamido-2-(diethylaminomethyl)phenol (14), 4,7-DCQ (5), and ADQ (3) were obtained in yields of 92, 89, and 90%, respectively. Costing and process mass intensities of 4,7-DCQ and ADQ are also reported.
Related Concept Videos
Preclinical Development: Overview
Drug Administration and Therapy Phases: Overview
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Factors Influencing Drug Absorption: Pharmaceutical Parameters
Clinical Trials: Overview

