Research Projects

The primary objective is to develop a cost-effective non-fringing synthetic route of Risdiplam, enhancing its efficacy and pharmacokinetic parameters. The RISDIPLAM synthesis is planned through a convergent process, involving the synthesis of Compound A B and coupling of Compound A B2 using a Pd-based catalyst. The synthesis of Compound A involves the aromatic nucleophilic substitution Boc-4,7-diazaspiro[2.5]octane with p-bromonitropyridine, which is reduced using a catalyst other than Rn-Ni/Pd-C. Compound D is cyclized using methyl dimethylmalonate in the presence of a suitable amphiphilic catalyst, yielding compound B. Compound A1 is synthesized by converting ethylacetoacetate to B1 in the presence of a non-nucleophilic base, which is then halogenated to yield compound A. Compound B2 is subsequently prepared using a bispinacolatodiborane pd catalyst. The drug formulation will be developed using a novel nanotechnology-based strategy using ultrasonication crystallization technique. The validation of the synthesized drug compound will be tested using cell-based assays to understand its ability to increase SMN protein levels. The development of a novel route of synthesis and formulation will reduce the cost of drug substance and formulation, ultimately reducing the burden on Indian populations, particularly infants and young children.