One‐potandtwo‐potmethods for chalcone derived pyrimidines synthesis and applications

Abstract

Chalcone-derived pyrimidine is a well-known heterocyclic compound that is commonly present in ribonucleic acid (RNA) and deoxyribonucleic acid (DNA) bio-isosteres. Pyrimidine derivatives are effective in both the electronic industry and drug industries. This review highlights the synthesis of pyrimidines, namely mono-pyrimidine, bis-pyrimidine, fused pyrimidine, symmetric, and asymmetric pyrimidine via one-pot and two-pot methods. The one-pot method is the direct reaction of amino derivatives with aldehydes and acetophenones, whereas the two-pot method is frequently reported for the synthesis of chalcone before the cyclization to a pyrimidine. This review is important in organic synthesis, particularly in the heterocyclic field, regarding pyrimidines and their significance in therapeutic and electronic industries.

Synthesis and evaluation of a new series of spiro aryl dioxolane compounds: A new scaffold as potential poly(ADP‐ribose)polymerase‐1 (PARP‐1) inhibitors

“…The expected pyrazoline 9 was not formed (Scheme 2). In addition, derivatives of pyrimidine have enormous extent of biological interest [42]. It is well known that pyrimidine ring systems have proved to be active as anti‐cancer and herbicidal agents [43, 44].…”

Chalcone derived benzoheterodiazepines for medicinal applications: A Two‐pot and one‐pot synthetic approach

“…The two-pot synthetic route has been efficiently reported in the preparation of hydroxy-substituted (8) derivatives with the aid of Ga(OTf) 3 to produce 30%-95% yield of products [131]. While multi-substituted benzodiazepine (9) was efficiently designed in the refluxing DMF with a few drops of piperidine as a catalyst. The screening for antibacterial and antifungal activities against Escherichia coli, Bacillus subtilis, Staphylococci aureus, Salmonella typhi, Aspergillus niger, Aspergillus fumigatus, Aspergillus oryzae, and Candida parapsilosis showed high antimicrobial potential for compounds 9b, 9h, and 9j with strong binding interactions toward B. subtilis, E. coli, and S. typhi (Scheme 2) [132].…”

“…Chalcone is a natural product [1] and bio-active [2,3] molecule that frequently used in the synthesis of heterocyclic compounds that is, pyrazole [4], imidazole [5,6], epoxide [7], benzodiazepine [8], pyrimidine [9], indole [10], flavone [11], isoflavone [12], and pyrazoline [13][14][15]. Chalcone-derived heterocyclic compounds consist of heteroatomic atoms (i.e., oxygen, sulfur, and nitrogen), which remarkable in the medicinal field for excellent activities in drug design [16][17][18].…”

Amino Derivatives of Diaryl Pyrimidines and Azolopyrimidines as Protective Agents against LPS-Induced Acute Lung Injury

“…The fact that the formation of a plane-conjugated fragment of a molecule bearing maximally distant hydrophilic groups at the ends, apparently, provides the most effective interaction with the binding sites of the target, according to a 3D molecular modeling. A wide range of biological activity is demonstrated by 4,6-diaryl substituted pyrimidines [ 9 ] derived from chalcones—a biologically important class of natural compounds [ 10 ]. A high pharmacological potential of 5,7-substituted [1,2,4]triazolo[1,5- a ]pyrimidines, including herbicidal, antifungal, antimalarial, antiviral, cardiovascular vasodilator, anti-inflammatory, analgesic, antimicrobial, and hypoglycemic activity, was demonstrated in the review [ 11 ].…”