Synthesis, Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives

Abstract

A new series of 5‐fluoro‐N4‐(3‐(4‐substitutedbenzylamino)phenyl)‐N2‐(4‐morpholinophenyl)pyrimidine‐2,4‐diamine derivatives (7a, 7b, 7c, 7d, 7e, 7f, 7g, 7h, 7i, 7j) are prepared from using an intermediate compound 5‐fluoro‐N4‐(3‐(aminophenyl)‐N2‐(4‐morpholinophenyl)pyrimidine‐2,4‐diamine (5). The structures of the newly synthesized products are established from their spectral 1H‐NMR, 13C‐NMR, 19F‐NMR, ESI‐MS, and analytical data. Here we report the synthesized compounds and larvicidal activity. All the compounds are screened for their significant larvicidal activity against third instar larvae at 24, 48, and 78‐h time exposure, and values were compared with standard drug Malathion. The Compounds 7i, 7a, 7c, 7f, and 7j exhibited significant activity. However the compounds 7b, 7e, 7d, and 7h showed excellent activity when compared to the above compounds and to standard drug malathion too because of the presence of mild electron withdrawing groups such as trifluoro, fluorine, hydroxy, nitro, and methoxy derivatives which are attached to the benzyl ring.

Facile One‐pot Synthesis of Arylsulfonyl‐4H‐pyrans Catalyzed by Ru Loaded Fluorapatite

“…In our continuous efforts to develop swift and green methodologies for the generation of novel heterocyclic molecules, earlier we have reported various highly efficient methods for synthesis of different condensed heterocyclic frameworks . We have also evaluated the biological activity of few series . The present protocol emphasizes the synthesis of new RuO 2 /FAp materials of different compositions and their scope as catalysts for preparation of novel arylsulfonyl‐4H‐pyrans in excellent yields, by the reaction of certain aromatic aldehydes, phenylsulphonyl acetonitrile and dimedone at room temperature with EtOH as green solvent.…”

Pyrimidine Derivatives: QSAR Studies of Larvicidal Activity against Aedes aegypti

“…Mosquitoes are a means of transmission of many neglected diseases, with millions of people being threatened vector-borne in the world, [1][2][3] particularly in tropical and subtropical regions. [4][5][6] According to Gorle et al, 7 these diseases affected chiefly the tropical and subtropical regions of countries that resist chemical vector control programs because the population refused to prevent mosquito control by using chemical treatment with synthetic insecticides. According to the World Health Organization (WHO), in recent years, the transmission of dengue hemorrhagic fever, zika virus, dengue fever and chikungunya has increased dramatically in those regions that are conducive to mosquito proliferation, as these mosquitoes adapt in environments characterized by irrigation systems and heavy rains.…”

“…According to the World Health Organization (WHO), in recent years, the transmission of dengue hemorrhagic fever, zika virus, dengue fever and chikungunya has increased dramatically in those regions that are conducive to mosquito proliferation, as these mosquitoes adapt in environments characterized by irrigation systems and heavy rains. [7][8][9][10][11][12] Chikungunya produces fever and rheumatic pain, interfering with people's quality of life for days, months or even years in more serious cases. Zika presents headache, irritation of the skin, redness of the eyes or vomiting, fatigue, fever, chills, loss of appetite or sweating.…”

Citric Acid/MCM‐48 Catalyzed Multicomponent Reaction: An Efficient Method for the Novel Synthesis of Quinoline Derivatives

“…Therefore, we continue our investigation for improving the efficiency, eco‐friendliness and green approach for the synthesis of various heterocycles . In recent past, we have stated few methodologies for the synthesis of different medicinal stimulating molecules . The current investigation lays emphasis on the synthesis of novel citric acid doped MCM‐48 solid material which was applied as a catalyst for the first time, and also its use in the synthesis of novel quinolines by the reaction of aromatic aldehydes, malononitrile, 5,5‐dimethylcyclohexane‐1,3‐dione and ammonium acetate at room temperature with EtOH as green solvent in excellent yields.…”