An article Direct Synthesis, Characterization and Theoretical Studies of N-(6-Amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)benzamide Derivatives WOS:000612107500027 published article about MONOXIDE-FREE AMINOCARBONYLATION; N-SUBSTITUTED FORMAMIDES; RECEPTOR KINASE 2; URACIL DERIVATIVES; AMIDE-BOND; DIRECT AMIDATION; ALCOHOLS; ARYL; NUCLEOSIDES; INHIBITION in [Das, Tushar; Das, Subrata] Natl Inst Technol Patna, Dept Chem, Patna 800005, Bihar, India; [Ranjan, Amit] Dr DY Patil Vidyapeeth, Dr DY Patil Biotechnol & Bioinformat Inst, Canc & Translat Res Lab, Pune 411033, Maharashtra, India; [Sieron, Leslaw; Maniukiewicz, Waldemar] Lodz Univ Technol, Inst Gen & Ecol Chem, Zeromskiego 116, Lodz, Poland; [Das, Tushar] Natl Inst Pharmaceut Educ & Res Hajipur, Dept Pharmacoinformat, Vaishali 844102, Hajipur, India in 2021, Cited 52. Product Details of 99-61-6. The Name is 3-Nitrobenzaldehyde. Through research, I have a further understanding and discovery of 99-61-6
With the far-flung importance of uracil and amides in innumerable fields of chemistry and biology, a coherent synthesis that nullifies the use of prodigal reagents, methods and catalysts are hugely accepted. From the present outcomes, we report a highly atom profitable nucleophilic addition reaction of aromatic aldehydes and heterocyclic amines for the generation of amides having an excellent yield and high reproducibility. The main force responsible for the forward reaction is the presence of the nitroso group at the C-5 position on uracil scaffold, which drives the formation of formidable range products. The conclusive mechanism is based on the dehydrogenation reaction of the carbinolamine product formed during the nucleophilic addition reaction of the aromatic aldehyde with the free heterocyclic amino group to yield the corresponding amides. The synthesized compounds were predicated for biological properties and proved it to be an ideal G protein-coupled receptor kinase2 (GRK2) inhibitor. Out of all, the compound 3 f showed the most preeminent properties when compared to Paroxetine, studied using molecular docking. At the same time, computed ADME analysis proved them as an ideal drug candidate. Our findings not only prophesize new methods for the synthesis of bioactive-amides using a cross-coupling strategy but also demonstrates their novel applications as a human GRK2 inhibitor.
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Reference:
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