The journey of a drug from discovery to market is paved with precisely synthesized chemical intermediates. One such critical compound is Ethyl 5-Amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate, known by its CAS number 256504-39-9. This chemical entity serves as a foundational component in the synthesis of important pharmaceuticals, most notably Riociguat, a medication vital for patients with pulmonary hypertension. Understanding its characteristics and sourcing is paramount for R&D scientists and procurement specialists in the pharmaceutical industry.

Key Properties and Pharmaceutical Relevance

Ethyl 5-Amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate is characterized by its molecular formula C13H14FN3O2 and a molecular weight of approximately 263.27 g/mol. It is typically supplied as an off-white to yellow solid with a high purity standard, often specified as ≥98.0%. This high purity is non-negotiable for pharmaceutical applications, as it directly impacts the success of subsequent synthetic steps and the quality of the final API. Its structure, incorporating a fluorinated aromatic ring and a pyrazole core, offers specific reactivity that makes it an ideal starting material for complex drug molecules like Riociguat.

The role of this intermediate in Riociguat synthesis is substantial. Riociguat is a potent stimulator of soluble guanylate cyclase (sGC), an enzyme that plays a crucial role in regulating vascular tone. By facilitating the synthesis of this drug, Ethyl 5-Amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate contributes directly to therapeutic advancements in cardiovascular medicine.

Procurement and Supplier Considerations

For pharmaceutical companies and contract manufacturing organizations (CMOs), securing a reliable supply of Ethyl 5-Amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate is a strategic priority. When looking to purchase this intermediate, several factors are crucial:

  • Supplier Reliability: Partnering with manufacturers known for consistent quality and adherence to Good Manufacturing Practices (GMP), where applicable, is essential.
  • Purity Standards: Always confirm that the product meets the ≥98.0% purity requirement and review the accompanying CoA.
  • Competitive Pricing: Research and obtain quotes from multiple suppliers to ensure cost-effectiveness, especially for large-scale orders.
  • Lead Times and Logistics: Understand the supplier's production capacity and shipping capabilities to ensure timely delivery and avoid production delays.

Many leading chemical manufacturers and suppliers are based in China, offering competitive pricing and extensive production capabilities for this intermediate. Direct engagement with these suppliers is often the most efficient way to obtain accurate quotes and discuss supply agreements.

Conclusion

Ethyl 5-Amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate is a linchpin intermediate in the pharmaceutical synthesis of Riociguat. Its reliable procurement, backed by stringent quality control and competitive pricing, is vital for pharmaceutical manufacturers. If your organization requires this chemical, exploring partnerships with established suppliers for purchase is a key step towards ensuring manufacturing continuity and product excellence.