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Synthesis, physico-chemical properties and microsomal stability of compounds bearing aliphatic trifluoromethoxy group
Journal of Fluorine Chemistry ( IF 1.7 ) Pub Date : 2020-01-17 , DOI: 10.1016/j.jfluchem.2020.109461
Ivan G. Logvinenko , Yevheniia Markushyna , Ivan S. Kondratov , Bohdan V. Vashchenko , Maria Kliachyna , Yuliya Tokaryeva , Valentyna Pivnytska , Oleksandr O. Grygorenko , Günter Haufe

Effects of the trifluoromethoxy substituent on physico-chemical properties of compounds, such as kinetic solubility, lipophilicity and microsomal clearance, was studied in a series of aliphatic derivatives. It was found that kinetic solubility of the CF3O-containing compounds was comparable to that of analogs, i.e. compounds bearing CH3O and CF3 moieties. The CF3O-substituted compounds had higher lipophilicity as compared to methoxy analogues, and nearly the same like CF3-bearing compounds. Microsomal stability studies indicated that the trifluoromethoxy group typically decreased metabolic stability of the corresponding derivatives as compared to either CH3O- or CF3-substituted counterparts, except for N-alkoxy(sulfon)amide series.



中文翻译:

带有脂肪族三氟甲氧基的化合物的合成,理化性质和微粒体稳定性

在一系列脂族衍生物中研究了三氟甲氧基取代基对化合物理化性质的影响,如动力学溶解度,亲脂性和微粒体清除率。发现含CF 3 O的化合物的动力学溶解度与类似物,具有CH 3 O和CF 3部分的化合物的动力学溶解度相当。与甲氧基类似物相比,CF 3 O-取代的化合物具有更高的亲脂性,并且与带有CF 3的化合物几乎相同。微粒体稳定性研究表明,与任一CH 3相比,三氟甲氧基通常会降低相应衍生物的代谢稳定性O-或CF 3取代的对应物,但N-烷氧基(磺)酰胺系列除外。

更新日期:2020-01-17
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