Synthesis of Pyridone Dioxoisoindoline and Carbamide Derivatives

Abstract

A pharmaceutical scientist must focus on developing cost effective, simple and newlinesustainable manufacturing process for both drug substance and drug product through newlinethorough optimization methodologies. The present research work aims at the newlinedevelopment of biologically active products with improved yields and high purity along newlinewith the synthetic approaches for their novel analogues. To achieve this, the reported newlinesynthetic routes for the biologically active products were reviewed and new approaches newlinewere designed for the synthesis of antiepileptic drug-Perampanel (Pyridone) analogues, newlineantipsoriatic arthritis-Apremilast (dioxoisoindoline) analogues, antiretroviral drug- newlineDarunavir and antipsychotic drug- Pimavanserin. newlineCHAPTER-1 newlineThis chapter describes about Significance of Process Research and newlineDevelopment in Active Pharmaceutical Ingredients . The development of a Medicine newlineis not an easy process and is Opaque. The time for an experimental medicine to travel to newlinethe stage of regulatory approval and patient reach is about 15 years and may costs about newline1.5 Bn USD. The drug development process mainly involves Discovery, Clinical and newlineRegulatory phases to reach the market. Once, the medicine reaches market, based on newlineincreased demand need of generic drug entry comes to make the medicine more newlineaffordable and reachable to the patients all over the world. newlineCHAPTER-2 newlineThis chapter describes the synthesis of pyridine-2(1H)-one analogues and newlineevaluating their anticancer activity. Inspired by the fact that 2-pyridone and its derivatives newlinehave significant biological activity, we have chosen substituted phenylpyridin-2(1H)-one newlinecore of Perampanel for our study. We have extended its carboxylic acid chain by forming newlineamide bond using an aromatic amine structure to improve the biological activity. And these derivatives were evaluated against anticancer activity.CHAPTER-3 newlineIn our study we focused on the synthesis of novel compounds by molecular newlinehybridization of the phthalimide ring with aromatic structures via CH=N linker. newline