NINGBO INNO PHARMCHEM CO.,LTD. is at the forefront of pharmaceutical intermediate synthesis, utilizing innovative biocatalytic cascade systems to produce key compounds like the sitagliptin intermediate. This advanced approach leverages the precision and efficiency of enzymes, offering a sustainable alternative to traditional chemical synthesis methods. Our focus on developing these cutting-edge processes is driven by the goal of delivering high-quality, cost-effective solutions for the pharmaceutical industry.

The synthesis of the sitagliptin intermediate, a critical component in the production of the popular type 2 diabetes medication Sitagliptin, has been significantly enhanced through our research into enzymatic cascade transaminase synthesis for sitagliptin. By employing a multi-enzymatic system that includes transaminase (TA), esterase, aldehyde reductase (AHR), and formate dehydrogenase (FDH), we can achieve high conversion rates. A key innovation in our approach is the use of benzylamine as an amino donor, which is significantly more cost-effective and readily available than other options. This choice directly contributes to lowering production costs and improving the overall economic viability of the process.

One of the primary challenges in enzymatic synthesis is managing enzyme inhibition by by-products. Our team has effectively addressed this by incorporating the AHR/FDH system to efficiently remove inhibitory by-products such as benzaldehyde. This strategic addition ensures the continuous activity of the transaminase, leading to higher overall yields and a purer final product. Furthermore, the integration of promoter engineering allows for precise control over the expression levels of each enzyme within a single whole-cell system. This fine-tuning optimizes the cascade's performance, ensuring maximum efficiency and productivity.

The ability to achieve excellent conversion rates, often exceeding 70-90% under optimized conditions, highlights the power of this biocatalytic process development. These advancements are crucial for meeting the growing global demand for diabetes treatments. NINGBO INNO PHARMCHEM CO.,LTD. is committed to driving innovation in green chemistry in pharmaceutical industry, and our work on the sitagliptin intermediate exemplifies this dedication. We continuously strive to refine our methodologies, ensuring that our products not only meet but exceed industry standards for quality, efficiency, and environmental responsibility.

As we look to the future, NINGBO INNO PHARMCHEM CO.,LTD. remains dedicated to exploring and implementing novel biocatalytic solutions for pharmaceutical synthesis. Our ongoing research into transaminase applications in pharma and the broader field of drug intermediate synthesis technologies aims to provide the pharmaceutical sector with the tools necessary for more sustainable and effective drug manufacturing.