An Easy Access to 4‐Trifluoromethylated 7‐(4‐Substitued‐1H‐1,2,3‐Triazol‐1‐yl)Pyrimido[1,2‐b]Pyridazin‐2‐One Systems

Abstract

Efficient synthesis of 7‐(1H‐1,2,3‐triazol‐1‐yl)‐4‐trifluoromethyl‐2H‐pyrimido[1,2‐b]pyridazin‐2‐ones from 7‐chloro‐4‐trifluoromethylpyrimido[1,2‐b]pyridazin‐2‐one by a consecutive SNAr reaction with azide, followed by copper‐catalyzed [3+2] cycloaddition is described.

Cu/Pd‐Catalyzed One‐Pot Synthesis of 2‐(1,2,3‐Triazolyl)methyl‐3‐alkynylImidazo[1,2‐a]pyridines Involving Sequential SN Reaction/[3+2] Cycloaddition/Sonogashira Coupling Reactions

“…No significant solvent effect was observed when the reaction took place in a polar aprotic solvent such as DMF (Table 2, entry 2). [19] Other catalysts were used, such as Cu(OAc) 2 ⋅ H 2 O, but no performance improvement was observed (Table 2, entry 3). Under the same reaction conditions and in the presence of triethylamine as base (3 equiv.…”

Molecular properties prediction, anticancer and anti-inflammatory activities of some pyrimido[1,2-b]pyridazin-2-one derivatives

“…Pyrimidines ability to inhibit the expression and activity of key inflammatory mediators such as prostaglandin E2, inducible nitric oxide synthase (iNOS), tumor necrosis factor-α (TNF-α), nuclear factor kappa B (NF-κB), as well as chemokines and cytokines, is believed to be the cause for its anti-inflammatory activity. 16 The current study addresses the cytotoxic and anti-inflammatory efficacy of eleven novel pyrimidine derivatives 17 based on trifluoromethylated pyrimido [1,2-b]pyridazin-2-one core substituted at position 7. The molecular mechanism underlying the anti-proliferative properties was studied by monitoring key apoptotic mediators and analyzing the cell cycle by flow cytometry.…”

“…The current study addresses the cytotoxic and anti-inflammatory efficacy of eleven novel pyrimidine derivatives 17 based on trifluoromethylated pyrimido[1,2-b]pyridazin-2-one core substituted at position 7. The molecular mechanism underlying the anti-proliferative properties was studied by monitoring key apoptotic mediators and analyzing the cell cycle by flow cytometry.…”