CASE STUDY:
Process Transfer and Optimization for an Anti-Cancer Agent

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.