Batch Synthesis of Primaquine Diphosphate Anti‐Malarial Drug

An improved three-step synthesis route toward Primaquine Diphosphate is reported herein. The anti-malarial drug was obtained via n-alkylation of readily available potassium phthalimide, followed by reductive amination and room temperature methylaminolysis-assisted phthalimido deprotection of the key intermediates to furnish Primaquine Diphosphate in 47% overall isolated yield.