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In the presence of Rh (II) catalyst, N-fluoroalkyl-1,2,3-triazole undergoes various denitrification transformations when heated in microwave. The reaction is carried out through Rh carbon reaction intermediates. Unlike N-trifluoromethyl secondary or tertiary amines, N-trifluoromethyl nitrogen heterocycles, such as pyrazole or benzimidazole, are stable in hydrolysis. These azoles exhibit excellent medicinal chemical properties, such as increased lipophilicity and CaCO2 permeability, no reactivity with glutathione, and reduced pKa, making them interesting building blocks in drug design. Although N-trifluoromethylazole is a rare compound, this part is beginning to appear in potential candidate drugs. For example, replacing the methyl substituent on nitrogen in trifluoromethyl checkpoint kinase 1 (CHK1) inhibitors leads to N-dealkylation inhibition while maintaining comparable inhibitory activity.
Norflo t-butyl ether is a typical representative of relatively hydrophobic high-intensity 19F nuclear magnetic resonance probes. Depending on whether the reporting team needs to reflect changes in the chemical environment near or far from the attachment point, short or medium length fluoroalkyl azides can be selected.
新氟化学
New Fluorine Chemical
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