NOVEL SYNTHETIC PROCESSES FOR THE INDUSTRIAL PREPARATION OF ACTIVE PHARMACEUTICAL INGREDIENTS

The project deals with the development of new synthetic processes for the industrial preparation of two emerging active pharmaceutical ingredients (API). Specifically, the process for the preparation of a new paclitaxel prodrug, namely octadecanedioc acid-paclitaxel, was defined. This paclitaxel derivate has shown better results in vivo trials, against a wide range of tumors, in terms of toxicity and efficacy, compared to other conventional formulations of PTX like Abraxane and Cremophor-EL. In order to have an easily scalable process and a final product with high purity a novel synthetic strategy was developed. The second part of the project focused on the development of a process for the industrial preparation of voclosporin, a semi-synthetic analogue of cyclosporin A. This new derivate has been approved for the immunosuppressant medication treatment of Lupus nephritis. A four synthetic steps process was developed to afford the product with the required purity and isomeric composition.