Executive Summary : | Eliglustat, a glucosylceramide synthase inhibitor, is being developed for long-term treatment of adult patients with Gaucher disease type 1. Cerdelga, developed by Genzyme Corp, has been approved by the FDA in August 2014. Clinical studies show that Eliglustat reduces the size of enlarged spleens and livers, with patients taking Cerdelga showing a 28 reduction in spleen size compared to placebo treatment. The proposed project aims to deliver Eliglustat synthesis under the photocatalytic method, reducing the number of steps and maintaining green technology. Formulation studies have also been proposed to improve the bioavailability of the drug. Genzyme Corporation has collaborated with two countries and six companies to develop the process and market worldwide. The significance of the project lies in making the drug more affordable and accessible. The project introduces emerging technology such as photocatalysis for the synthesis of C-N bond formation, which is a special place in organic synthesis. The Gabriel method is a classical method for transforming alkyl halide into substituted amines without any poly alkylation. Photocatalysis offers advantages such as mild reaction conditions, ambient temperatures, good selectivity, and reactivity. The key step in the proposal is locking adjacent carbon atoms stereochemistry in syn fashion via DyKAT asymmetric reductions. The project also proposes a cost-effective formulation process, including pre-formulation studies, analytical method development, formulation development and optimization, and characterization of the developed formulation. |