Synthesis and biological screening of diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates was written by Olawode, Emmanuel O.;Tandlich, Roman;Prinsloo, Earl;Isaacs, Michelle;Hoppe, Heinrich;Seldon, Ronnett;Warner, Digby F.;Steenkamp, Vanessa;Kaye, Perry T.. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2018.Reference of 2103-99-3 This article mentions the following:
A three-step synthesis, involving condensation of bromomethyl aryl ketones with urea to afford 2- aminothiazoles, their chloroacetylation and subsequent solvent-free Arbuzov phosphonation has afforded a series of novel di-Et [N-(thiazol-2-yl)carbamoyl]methylphosphonates 3a–3f in good overall yields; the 4- carboxythiazole analog 3g was obtained by selective hydrolysis of the corresponding Et ester 3f. The phosphonate esters exhibited significant anti-cancer activity (nM – low μM IC50 values) against SH-SY5Y cells and, in one case, 7.6μM MIC90 anti-TB activity against the virulent M. tuberculosis H37Rv strain; the chloroacetamido precursors all exhibited some antimalarial (PfLDH) activity, three with IC50 values in the range 1.0 – 8.9μΜ. In the experiment, the researchers used many compounds, for example, 4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3Reference of 2103-99-3).
4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 2103-99-3
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica