Case Study 1:  Process Transfer and Optimization

Cedarburg Hauser Pharmaceuticals was contracted to transfer and optimize the synthetic process for a new anti-cancer agent undergoing clinical trials. The existing route to an intermediate involved numerous isolations and required an inefficient high temperature reaction. Cedarburg was able not only to telescope the synthetic sequence into “one pot” and avoid isolation of the intermediate, but also developed a new lower temperature ring formation affording the intermediate in higher yields and purity. Further improvements to the synthesis involved replacing expensive and not readily available reagents with commercially available less expensive ones, and the elimination of one of the expensive and toxic solvents used in the process. Overall, Cedarburg was able to almost double the output of the existing synthetic route utilized in producing the final API and provided substantial cost savings to our customer.

Case Study 2: New Process Development

Cedarburg Hauser Pharmaceuticals was contracted to develop a process for a key intermediate in the flavor industry with the criteria that the process eliminate a complex chromatography, be scalable to metric tons, and reduce 100-fold the cost per kilogram. Cedarburg was able to significantly improve a literature procedure which replaced elemental sulfur chemistry with a mercaptan variant and substantially improved the process. We eliminated chromatography, significantly reduced processing time, simplified purification, removed lingering odor and coloration issues, met the original price objectives and provided material of greater than 99% assay in good yields, thereby meeting or exceeding all of the original project goals.

Case Study 3: New Process Development

Cedarburg Hauser Pharmaceuticals was contracted for the development and validation of a new synthetic process for a commercially available prostaglandin. The existing process was tedious, and required multiple steps, isolations and purifications. In addition to reducing the overall number of synthetic steps and introducing efficiencies that made the synthesis significantly more cost-effective, a thorough understanding of the process enabled the implementation of process controls that simplified purification. Modifying the workups enabled the removal of two of the three chromatographies reducing the number to a single high yielding normal phase chromatographic process and producing material that exceeded our customer's target specifications.

Case Study 4: Enhancement and Isolation Process Development of a Natural Product

Cedarburg Hauser Pharmaceuticals was contracted to develop a scalable process for the isolation of a naturally occurring target molecule, a potential therapeutic for the treatment of Alzheimer’s disease. The natural abundance of the target compound in the biomass extract was less than 0.05% and the existing mg scale route required several chromatography steps requiring semi-preparative HPLC columns. Cedarburg Hauser was able not only to develop an isolation process scalable to kilogram quantities of the target compound, but also developed methodology to enhance the compound of interest by 7-fold from a precursor compound already present in the natural source.