首页> 外国专利> IMIDAZOLINE 8-HEXYLOXYPHENYL-2-IMIDAZOLINE, 8-NONYLOXYPHENYL-2-IM IDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND OBTENTION PROCESS.

IMIDAZOLINE 8-HEXYLOXYPHENYL-2-IMIDAZOLINE, 8-NONYLOXYPHENYL-2-IM IDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND OBTENTION PROCESS.

机译:咪唑啉8-己氧基苯-2-咪唑啉,8-壬氧基苯-2-咪唑啉和7-壬氧基苯-2-咪唑啉和7壬氧基苯-2-咪唑啉和合成过程。

摘要

The present invention is related to the compounds 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE and process for obtaining same. These compounds are obtained by a two-step process: an alkylation of 3ùhydroxybenzaldehyde with the corresponding alkyl halide obtaining 81% of isolated yield and a cyclization performed by ethylenediamine, potassium carbonate, triethylamine, iodine and t-butanol, obtaining quantitative yield. Both compounds, 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE, have in vitro activity against Tripanosoma cruzi; the compounds have been evaluated over blood Trypomastigote from the NINOA and INC-5 strains, in the latter strain presenting an activity practically equal to the drugs of clinical use Nifortimox and Benznidazol at concentrations of 19.2 and 38.4 ÁM. The compounds 7-NONYLOXYPHENYL-2-IMIDAZOLINE AND 7-NONYLOXYPHENYL-2-IMIDAZOLINE, due to the chemical characteristics thereof could lead to molecular gels, which are formed by nanoparticles.
机译:本发明涉及化合物7-壬基氧苯基-2-咪唑啉和7-壬基氧苯基-2-咪唑啉及其制备方法。这些化合物可通过两步过程获得:将3-羟基苯甲醛与相应的烷基卤进行烷基化,获得81%的分离产率;通过乙二胺,碳酸钾,三乙胺,碘和叔丁醇进行环化,获得定量的产率。 7-NONYLOXYPHENYL-2-咪唑啉和7-NONYLOXYPHENYL-2-咪唑啉这两种化合物均具有体外抗克氏锥虫活性。该化合物已从NINOA和INC-5菌株的血锥虫中进行了评估,在后者中,其活性与临床上Nifortimox和Benznidazol的浓度分别为19.2和38.4ÁM的药物几乎相同。化合物7-壬基氧基苯基-2-咪唑啉和7-壬基氧基苯基-2-咪唑啉由于其化学特性可能会导致由纳米粒子形成的分子凝胶。

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