An activation of methyl ketones or active methylenes and N, Ndimethylformamide dimethyl acetal at 110 °C by sulfated polyborate under solvent-free conditions has been developed for enamines and enaminones synthesis. Selected Brønsted acid, optimized reaction conditions, and easy separation method lead to 82-97 % yield, making this process costeffective and eco-friendly. We chose boric acid for scale-up activity in the interest of readers and industries. The optimized reaction condition was applied to demonstrate a 10 gram scale for the intermediate of Imatinib and Nilotinib with an 80 % from 3-acetylpyridine. This method is extendable to produce Ocinaplon intermediate with 80.6 % yield using 4-acetyl pyridine as starting material.
An activation of methyl ketones or active methylenes and N,N-dimethylformamide dimethyl acetal (DMF-DMA) at 110 °C by sulfated polyborate under solvent-free conditions has been developed for enamines and enaminones synthesis. Selected Brønsted acid, optimized reaction conditions, and easy separation method lead to 82-97% yield, making this process cost-effective and eco-friendly. We chose boric acid for scale-up activity in the interest of readers and industries. The optimized reaction condition was applied to demonstrate a 10 gm scale-up for intermediate of Imatinib and Nilotinib with 80% yield from 3-acetylpyridine. This method is extendable to produce Ocinaplon intermediate using 4-acetyl pyridine as starting material.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.