Improved Process for Centhaquine

• High yield: >90% (current method) vs. 47% or 71% (previous methods)
• Lower estimated raw material cost: ~$224/kg
• Higher purity: Results in reduced purification costs

• An improvement over previously reported processes for the preparation.
• An atom-economical and greener approach for the synthesis of Centhaquin and Centhaquin citrate by replacing previously reported acidic conditions.
• Aqueous, catalyst-free, high-yielding, and column chromatography-free process, fully optimized at the multigram scale (>50 g across three batches), with complete characterization of the API and related impurities.

• High yield: >90% (current method) vs. 47% or 71% (previous methods)
• Lower estimated raw material cost: ~$224/kg
• Higher purity: Results in reduced purification costs
• Green credentials:

• Aqueous synthesis
• Room temperature operation
• Lower E-factor

• Scalability: Optimized at >50 g scale across three batches
• Comprehensive analysis: Complete characterization of the API and related impurities
• Salt preparation: Successfully prepared the citrate salt