Synthesis of Flavones From 2-Hydroxy Acetophenone and Aromatic Aldehyde Derivatives by Conventional Methods and Green Chemistry Approach

Abstract

Objective: Flavones occupy a special place in the realm of natural and synthetic organic chemistry owing to their diversified biological activities. In this study, a series of chalcone derivatives were synthesized and after cyclization of chalcone to synthesized various substituted flavone derivatives (2A-2L). Methods:The reaction of 2-hydroxy acetophenone with substituted aromatic aldehydes produced chalcone by trituration (NaOH) and conventional methods (KOH/EtOH), which upon further cyclization with dimethyl sulfoxide/I 2 resulted to form flavone derivatives. Results:The purity of compounds was ascertained by melting point and thin-layer chromatography. The synthesized compounds have been characterized by mass, infrared, and 1 H nuclear magnetic resonance spectral analysis. Conclusion:Based on spectral data, it was proved that all synthesized chalcones and flavones derivatives meet the standard values of various spectral techniques and further it will be evaluated for pharmacological activities.

Synthesis and Evaluation of 1,3,5-Triaryl-2-Pyrazoline Derivatives as Potent Dual Inhibitors of Urease and α-Glucosidase Together with Their Cytotoxic, Molecular Modeling and Drug-Likeness Studies

“…The spectral data of previously reported 2′-hydroxychalcones (1a–1q) are given in the following reference articles 1a, 1e , 1g, 1j , 1b , 1c , 1d , 1f , 1h , 1i , 1k , 1l , 1m , 1n , 1o , 1p and 1q . The spectral data of all the synthesized pyrazolines ( 2a–2q) are given here:…”

Prepare several substituted pyridines derived from Chalcone and evaluate their bioactivity

“…Also, interest has increased in the use of Chalcone for the purpose of developing many antibacterial compounds (17) (18) , anti-ulcer, (19) antimicrobial (20) (21) , gave activity against three types of human cancer cells (HepG2) liver, (HCT116) colon, (MCF-7) breast (22) , Chalcone chemistry is still a source of great interest For scientists in the 21st century, a variety of promising drugs were produced, such as antifungals (23) (24) , anti-inflammatory, (25) (26) , antitumor (27) , anti-diabetic (28) (29) , Also among the examples of compounds in which the Chalcone derivative is included is a compound (2) anti-genetic and cytotoxic (30) , a compound (3) anti-inflammatory (32) (31) The first pyrimidine derivative (23) was isolated in the year (1818) and is alloxan by the scientist (Brugnatelli) (33) by oxidation of uric acid and nitric acid. Pyrimidine has three isomers that depend on the positions of the two nitrogen atoms in the hexagonal ring (34) , and they have a structure similar to the pyridine ring in that they contain a hexagonal ring and a nitrogen atom (35) , If the substitution is in position 1,2, it is known as pyridazine, at position 1,3 it is known as pyrimidine, and at position 1,4 it is known as pyrazine (36) (37) . The interest in pyrimidine derivatives has also increased in the past years because they give a wide range of biological activities such as antibacterial, antifungal, antihypertensive, heart disease, bronchodilator or antitumor activity.…”

Synthesis novel flavone from vanillin

“…Therefore, using available chemical materials, an alternative to obtaining Flavone compounds with greater yields is taken from the synthesis method. Such as the synthesis of Flavones from 2-hydroxyarylchalcones by Patel and Shah [14], Flavones from 2'-alyloxy-α, βdibromochalcone and iodides [15], Flavones from o-benzyloxyacetophenone as therapy (anti-diabetic, anti-inflammatory, antioxidant, and anti-cancer) [16].…”