Abstract:The catalyst-free reactions of Baylis-Hillman alcohols (1a-i) with 2-aminobenzimidazole (2) in THF-H 2 O (1:4) were developed for the convenient and greener synthesis of benzimidazo[1,2-a]pyrimidinone derivatives (3a-i). The pesticidal activities of 3a-i were examined to investigate a new biological activity of the imidazo[1,2-a]pyrimidinone-type compounds.aqueous media, Baylis-Hillman alcohol, 2-aminobenzimidazole, pesticidal activity
“…Pyrimidobenzimidazoles 129 were evaluated for pesticidal activity. 75 Derivatives 129a – d were the most active against Plutella xylostella at a concentration of 100 mg/ml with a lethality of 70–90%. At a concentration of compounds 129a – d of 500 mg/ml, the lethality against Tetranychus cinnabarinus was 100% (Table 12 ).…”
Section: Biological Activity Of Pyrimidobenzimidazole Derivativesmentioning
confidence: 99%
“…Wong and colleagues presented a series of publications on the synthesis of pyrimidobenzimidazoles 127 , 129 , 131 via the reaction of 2-aminobenzimidazole ( 1а ) with Baylis–Hillman acetates, alcohols, and amines 126 , 128 , 130 , respectively. 75 – 77 The methods presented by the authors assume varying conditions, catalysts, and reagents (Scheme 32 ). Scheme 32 …”
Section: The Reaction Of Aminobenzimidazoles With Bifunctional Synthetic Equivalentsmentioning
Nitrogen-containing heterocyclic compounds are the basis of many natural and synthetic biologically active substances. 1 More than two-thirds of the known drugs used in clinical practice contain heterocyclic and, above all, nitrogen-containing fragments within their structure. Over the past decades, the chemistry of aza-heterocycles has received considerable attention due to the wide spectrum of their biological activity and numerous therapeutic applications in medicine.Of nitrogenous heterocycles, azoloazines containing fragments similar to the natural heterocycles purines and pyrimidines are currently of great practical importance. Thus, non-natural nucleosides abacavir, famciclovir, remdesivir are known, which are the products of structural modifications of all the components of the nucleotide exhibiting excellent indicators of antiviral action (Fig. 1). [2][3][4] In addition to the generally accepted nucleoside forms, the azoloazines themselves are relevant in the search for means of combating diseases on a global scale. Nitroazolo- [5,1-c][1,2,4]triazines and nitroazolo [1,5-a]pyrimidines, a new family of antiviral compounds has been found. 5 The
“…Pyrimidobenzimidazoles 129 were evaluated for pesticidal activity. 75 Derivatives 129a – d were the most active against Plutella xylostella at a concentration of 100 mg/ml with a lethality of 70–90%. At a concentration of compounds 129a – d of 500 mg/ml, the lethality against Tetranychus cinnabarinus was 100% (Table 12 ).…”
Section: Biological Activity Of Pyrimidobenzimidazole Derivativesmentioning
confidence: 99%
“…Wong and colleagues presented a series of publications on the synthesis of pyrimidobenzimidazoles 127 , 129 , 131 via the reaction of 2-aminobenzimidazole ( 1а ) with Baylis–Hillman acetates, alcohols, and amines 126 , 128 , 130 , respectively. 75 – 77 The methods presented by the authors assume varying conditions, catalysts, and reagents (Scheme 32 ). Scheme 32 …”
Section: The Reaction Of Aminobenzimidazoles With Bifunctional Synthetic Equivalentsmentioning
Nitrogen-containing heterocyclic compounds are the basis of many natural and synthetic biologically active substances. 1 More than two-thirds of the known drugs used in clinical practice contain heterocyclic and, above all, nitrogen-containing fragments within their structure. Over the past decades, the chemistry of aza-heterocycles has received considerable attention due to the wide spectrum of their biological activity and numerous therapeutic applications in medicine.Of nitrogenous heterocycles, azoloazines containing fragments similar to the natural heterocycles purines and pyrimidines are currently of great practical importance. Thus, non-natural nucleosides abacavir, famciclovir, remdesivir are known, which are the products of structural modifications of all the components of the nucleotide exhibiting excellent indicators of antiviral action (Fig. 1). [2][3][4] In addition to the generally accepted nucleoside forms, the azoloazines themselves are relevant in the search for means of combating diseases on a global scale. Nitroazolo- [5,1-c][1,2,4]triazines and nitroazolo [1,5-a]pyrimidines, a new family of antiviral compounds has been found. 5 The
“…Among the twelve principles, safer and green solvents have been recognized as one of the most important and indispensable elements in the current chemical society. 2,3 Compared with the commonly toxic and highly volatile solvents, some green and sustainable solvents such as supercritical fluids, 4 ionic liquids, 5 and water, 6 have been intensively studied from the beginning of the 21st century. It is noteworthy that water as a green and sustainable reaction medium has received increasing attention from the synthetic community.…”
Aromatic α-aminoazaheterocycles are the focus of significant investigations and exploration by researchers owing to their key role in diverse biological and physiological processes.
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