Abstract
An efficient and practical protocol has been developed to synthesize dihydropyrimidinones and dihydropyrimidinethiones through FeCl3∙6H2O/TMSBr-catalyzed three-component cyclocondensation under microwave irradiation. This approach features high yields, broad substrate scope, short reaction time, mild reaction conditions, operational simplicity and easy work-up, thus affording a versatile method for the synthesis of dihydropyrimidinones and dihydropyrimidinethiones.
Highlights
Dihydropyrimidinones and dihydropyrimidinethiones have received great attention in synthetic organic chemistry because of their ubiquitous presence in a large number of natural products and pharmaceutical agents [1–10]
Dihydropyrimidinones display as a key precursor in the synthesis of pyrimidine bases which constitute the basic skeleton of nucleic acids [30]
We began our study by investigating the reaction of 1-tetralone (1a), benzaldehyde (2a) and thiourea (3a) in CH3 CN at 90 ◦ C in an oil bath for 10 h employing FeCl3 ·6H2 O as the
Summary
Dihydropyrimidinones and dihydropyrimidinethiones have received great attention in synthetic organic chemistry because of their ubiquitous presence in a large number of natural products and pharmaceutical agents [1–10] They act as key components in natural marine alkaloids such as batzelladine A-I [11–13], ptilocaulin [14], and saxitoxin [15]. They exhibit a broad spectrum of pharmacological activities such as antibacterial [16], antitumor [17–20], anti-inflammatory [20], antiviral [21], and antihypertensive activities [22,23]. Dihydropyrimidinones display as a key precursor in the synthesis of pyrimidine bases which constitute the basic skeleton of nucleic acids [30]. An efficient access to these two structures is highly desirable for both organic synthesis and drug discovery
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