75129-08-7Relevant academic research and scientific papers
One pot synthesis of pyrimidine-5-carbonitrile and pyrimidine-5-carboxamide using ammonium chloride under solvent free condition
Aher,kardel,Gaware,Lokhande,Bhagare
, (2019/07/02)
Abstract: Pyrimidine-5-carbonitrile and pyrimidine-5-carboxamide were synthesized from the various substituted benzaldehyde, malononitrile and cyanoacetamide, urea/thiourea in the presence of ammonium chloride followed by characterization using IR, 1
Agonists for the adenosine A1 receptor with tunable residence time. a case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines
Louvel, Julien,Guo, Dong,Agliardi, Marta,Mocking, Tamara A. M.,Kars, Roland,Pham, Tan Phát,Xia, Lizi,De Vries, Henk,Brussee, Johannes,Heitman, Laura H.,Ijzerman, Adriaan P.
supporting information, p. 3213 - 3222 (2014/05/20)
We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines as selective human adenosine A 1 receptor (hA1AR) agonists with tunable binding kinetics, this without affecting their nanomolar affinity for the target receptor. They show a very diverse range of kinetic profiles (from 1 min (compound 52) to 1 h (compound 43)), and their structure-affinity relationships (SAR) and structure-kinetics relationships (SKR) were established. When put in perspective with the increasing importance of binding kinetics in drug discovery, these results bring new evidence of the consequences of affinity-only driven selection of drug candidates, that is, the potential elimination of slightly less active compounds that may display preferable binding kinetics.
Reactions with Substituted Acrylonitriles: A Novel Synthesis of Polysubstituted Pyrimidines
El-Sharabsy, Salwa A.,Gawad, Soad M. Abdel,Hussain, Sohair M.
, p. 207 - 211 (2007/10/02)
3-Arylacrylonitrile-2-thiocarboxamides (1a - d) reacted with S-methylisothiourea to give 4-amino-6-aryl-2-methylmercaptopyrimidine-5-carbonitriles (3a - d).The products 3a - d were also obtained via the reaction of 3-arylacrylonitrile-2-carbonitriles (4a
