Scaling up biocatalytic processes from laboratory bench to industrial production presents unique challenges. At NINGBO INNO PHARMCHEM CO.,LTD., we have successfully navigated these complexities in the manufacturing of the sitagliptin intermediate, a critical component in antidiabetic medication. Our strategic approach integrates robust enzymatic cascade systems with meticulous process optimization, demonstrating the viability and efficiency of biocatalysis for large-scale pharmaceutical production.

The production of the sitagliptin intermediate requires precise biochemical transformations. Our methodology relies on a multi-enzymatic cascade system featuring transaminases and esterases, enhanced by efficient cofactor regeneration. A cornerstone of our success in scaling up this sitagliptin intermediate synthesis is the use of benzylamine as a cost-effective amino donor. This selection, combined with our ability to manage enzyme inhibition through auxiliary enzymes like AHR and FDH, ensures high conversion rates and product purity even at larger scales.

Key to our scaling strategy is the implementation of advanced enzyme engineering techniques, particularly promoter engineering. This allows us to precisely control the expression levels of individual enzymes within a single whole-cell biocatalyst. By balancing the activity of enzymes such as transaminases and esterases, we optimize the entire cascade for maximum efficiency and productivity. This approach to biocatalytic process development has been instrumental in achieving consistent and high yields of the sitagliptin intermediate.

Furthermore, our research into drug intermediate synthesis technologies emphasizes sustainable practices. By utilizing biocatalysis, we significantly reduce the environmental footprint associated with traditional chemical synthesis. This includes minimizing the use of hazardous solvents and reagents, and lowering energy consumption. NINGBO INNO PHARMCHEM CO.,LTD. is committed to driving the adoption of such green methodologies across the pharmaceutical manufacturing sector.

The successful scale-up of our biocatalytic process for the sitagliptin intermediate underscores the immense potential of enzymes in modern manufacturing. NINGBO INNO PHARMCHEM CO.,LTD. is proud to be at the forefront of this evolution, providing the pharmaceutical industry with high-quality intermediates through efficient, sustainable, and scalable biocatalytic solutions. Our ongoing commitment to innovation ensures we continue to deliver value and advance the field of pharmaceutical chemistry.