Project Goal:

Synthesis of several advanced intermediates on 0.5-1 kg scale

Details:

A customer began a relationship with CalChem by requesting to synthesize four different advanced intermediates needed for their drug discovery program and API development.  The customer provided medicinal chemistry procedures for three of the compounds which were performed on mg scales and required major process modifications for the scale up.

No process for the synthesis of the fourth intermediate was provided.

Outcome:

CalChem began to evaluate the provided synthetic routes and was able to optimize each process to make 0.5-1 kg of the first three intermediates in an average of five steps.  For the last intermediate, an extensive literature search was conducted and a synthetic route was identified to make the molecule in a sequence of three steps.  0.5 kg of this compound was successfully prepared and fully characterized by the available analytical methods.  All these four intermediates were synthesized in high purity and delivered to the customer in less than four months.