Abstract
Enaminones, 4-methyl-1-[4-(piperazin/morpholin-1-yl) phenyl] pent-2-en-1-one (IIa–b) were synthesized by refluxing 1-[4-(piperazin/morpholin-1-yl) phenyl] ethan-1-one (Ia–b) with dimethylformamide dimethylacetal (DMF–DMA) without any solvent. The three dimensional structure of enaminone (IIb) containing morpholine moiety was confirmed by single crystal X-ray crystallography. Finally, the dihydropyrimidinone derivatives (1–20) were obtained by reacting enaminones (IIa–b) with urea and different substituted benzaldehydes in the presence of glacial acetic acid. Dihydropyrimidinone derivatives containing piperazine/morpholine moiety were synthesized in a good yield by means of simple and efficient method.
Highlights
Pyrimidines scaffold have played a significant role in the area of medicinal chemistry [1].Pyrimidines are important moieties because of their potential biological activities such as antitumor, antiviral, and antibacterial agents [2,3]
Dihydropyrimidinone compounds were first synthesized by Pietro Biginelli
Dihydropyrimidinones have emerged as calcium channel blockers and antihypertensive agents [7]
Summary
Pyrimidines scaffold have played a significant role in the area of medicinal chemistry [1]. Dihydropyrimidinones have emerged as calcium channel blockers and antihypertensive agents [7] These compounds exhibit a broad range of pharmacological activities, such as antibacterial, antitumor, antiviral, and anti-inflammatory [8]. Many potent marketed drugs like fluphenazine, cinnarizine, flunarizine, lomerizine, ciprofloxacin, indinavir, etc., have a piperazine moiety (Figure 1). Molecules 2018, 23, 1559 potent marketed drugs like fluphenazine, cinnarizine, flunarizine, lomerizine, ciprofloxacin, indinavir, etc., have a piperazine moiety (Figure 1). Morpholine is an organic moiety containing nitrogen and oxygen in a heterocyclic six-membered ring, and is considered as an important building block in the field of medicinal chemistry. The literature review suggested that molecules possessing these important scaffolds The literature review suggested that molecules possessing these important scaffolds (piperazine/morpholine and dihydropyrimidinone) may have significant therapeutic activity.
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