Application In Synthesis of Ethyl propiolateIn 2021 ,《Design, synthesis and biological evaluation of new thiazole scaffolds as potential TRPM8 antagonists》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Marsicano, Vincenzo; Arcadi, Antonio; Bianchini, Gianluca; Tomassetti, Mara; Aramini, Andrea. The article contains the following contents:
The preliminary results on the development of a viable methodol. for the further functionalization of 4-hydroxythiazole derivatives to afford target TRPM8 antagonists are reported. The combined Sonogashira coupling/annulation reactions of the Et 2-(3-fluorophenyl)-4-tifluoromethylsulfonyloxy-1,3-thiazole-5-carboxylate have been applied to the synthesis of analogs of the selective blocker of TRPM8 DFL23448. Among all the synthetised derivatives, the most promising compound resulted to be active as TRPM8 blocker (IC50 = 4.06 μM), showing an excellent metabolic stability and no cytotoxic effects. Finally, in silico characterization of the derivatives showed no violation of the drug-likeness rules. In the part of experimental materials, we found many familiar compounds, such as Ethyl propiolate(cas: 623-47-2Application In Synthesis of Ethyl propiolate)
Ethyl propiolate(cas: 623-47-2) is a clear colorless to pale yellow liquid that is soluble in ethanol, ether and chloroform. It an important organic chemical raw material and pharmaceutical intermediate. Ethyl propargylate is obtained by oxidation of propargyl alcohol to propargylic acid followed by esterification.Application In Synthesis of Ethyl propiolate
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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics