Abstract
An efficient synthesis of novel 2,3-dihydro-4H-pyrido[1,2-a]pyrimidin-4-ones has been reported. Inexpensive and readily available substrates, environmentally benign reaction condition, and product formation up to quantitative yield are the key features of this methodology. Products are formed by the aza-Michael addition followed by intramolecular acyl substitution in a domino process. The polar nature and strong hydrogen bond donor capability of 1,1,1,3,3,3-hexafluoropropan-2-ol is pivotal in this cascade protocol.
Highlights
The 1,3-nitrogenous bicyclic frameworks have been illustrious in drug discovery
From literature survey it was apparent that there are no reports on the dihydropyrido-pyrimidinones chemistry and their biological activity
Engage in small molecule research, we wanted to explore the synthesis of dihydropyrido-pyrimidinones and their biological activities
Summary
Many pyrido-pyrimidinone scaffolds (i.e., Fig. 1) have occupied privileged position in medicinal chemistry due to their unprecedented biological activities. It is a key constituent of numerous natural products possessing wide range of therapeutic properties including antitumor, anti-influenza, oxidative burst inhibition, lipid droplet synthesis inhibition, and anti-obesity properties[1,2,3,4,5,6,7,8,9,10]. Zeng et al have utilized palladium catalyzed C-H activation entailed carbonylative cycloamidation of ketoimines (Fig. 3, Case A)[17]. We present our results involving sustainable design and catalyst free synthesis of 2,3-dihydro-4H-pyrido[1,2-a] pyrimidin-4-one derivatives
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
