The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 1722-12-9, formula is C4H3ClN2, Name is 2-Chloropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Computed Properties of 1722-12-9.
Ramdas, Vidya;Talwar, Rashmi;Kanoje, Vijay;Loriya, Rajesh M.;Banerjee, Moloy;Patil, Pradeep;Joshi, Advait Arun;Datrange, Laxmikant;Das, Amit Kumar;Walke, Deepak Sahebrao;Kalhapure, Vaibhav;Khan, Talha;Gote, Ganesh;Dhayagude, Usha;Deshpande, Shreyas;Shaikh, Javed;Chaure, Ganesh;Pal, Ravindra R.;Parkale, Santosh;Suravase, Sachin;Bhoskar, Smita;Gupta, Rajesh V.;Kalia, Anil;Yeshodharan, Rajesh;Azhar, Mahammad;Daler, Jagadeesh;Mali, Vinod;Sharma, Geetika;Kishore, Amitesh;Vyawahare, Rupali;Agarwal, Gautam;Pareek, Himani;Budhe, Sagar;Nayak, Arun;Warude, Dnyaneshwar;Gupta, Praveen Kumar;Joshi, Parag;Joshi, Sneha;Darekar, Sagar;Pandey, Dilip;Wagh, Akshaya;Nigade, Prashant B.;Mehta, Maneesh;Patil, Vinod;Modi, Dipak;Pawar, Shashikant;Verma, Mahip;Singh, Minakshi;Das, Sudipto;Gundu, Jayasagar;Nemmani, Kumar;Bock, Mark G.;Sharma, Sharad;Bakhle, Dhananjay;Kamboj, Rajender Kumar;Palle, Venkata P. research published 《 Discovery of Potent, Selective, and State-Dependent NaV1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides》, the research content is summarized as follows. Voltage-gated sodium channel NaV1.7 is a genetically validated target for pain. Identification of NaV1.7 inhibitors with all of the desired properties to develop as an oral therapeutic for pain has been a major challenge. Herein, we report systematic structure-activity relationship (SAR) studies carried out to identify novel sulfonamide derivatives as potent, selective, and state-dependent NaV1.7 inhibitors for pain. Scaffold hopping from benzoxazine to chroman and indane bicyclic system followed by thiazole replacement on sulfonamide led to identification of lead mols. with significant improvement in solubility, selectivity over NaV1.5, and CYP2C9 inhibition. The lead mols. 13, 29, 32, 43, and 51 showed a favorable pharmacokinetics (PK) profile across different species and robust efficacy in veratridine and formalin-induced inflammatory pain models in mice. Compound 51 also showed significant effects on the CCI-induced neuropathic pain model. The profile of 51 indicated that it has the potential for further evaluation as a therapeutic for pain.
Computed Properties of 1722-12-9, 2-Chloropyrimidine is a monochlorinated pyrimidine with plant growth regulating activity. Chloropyrimidine is a useful reagent in the preparation of antivirals and other biologically active compounds.
2-Chloropyrimidine undergoes cobalt-catalyzed cross-coupling reaction with aryl halides.
2-Chloropyrimidine is a molecule that can be synthesized by the oxidation of pyrimidine with hydrogen peroxide and hydrochloric acid. The reaction proceeds through an electrochemical process in which the oxidation catalyst is a platinum electrode. This reaction is catalyzed by the nucleophilic attack of malonic acid on the chloropyrimidine at the methylene group. This efficient method for making 2-chloropyrimidine has been applied to synthesize aryl halides, including phenyl chloropyrimidine and pyridyl chloropyrimidine, from their corresponding chloride and bromide precursors. The fluorescence properties of 2-chloropyrimidine have been studied in coordination chemistry, where it forms complexes with metal ions such as Mn2+. In this study, it was found that adsorption mechanisms are dependent on molecular size, charge density, kinetic energy, and adsorbent surface area., 1722-12-9.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia