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METHOD FOR PREPARING PHENYL-SUBSTITUTED DERIVATIVES OF PYRIDINE LABELED WITH TRITIUM

机译:RIT标记的吡啶取代苯酚衍生物的制备方法

摘要

FIELD: organic chemistry, chemical technology.;SUBSTANCE: invention relates to a method for preparing N-phenylpicolinium salts and phenyl-substituted picolines labeled with tritium by phenyl ring of the general formula: [CH3C5H4N+C6H* 5]BF- 4 and CH3C6H* 5C5H3N. Method involves arylation of 2-, 3- and 4-picolines with free phenyl cations obtained in beta-decay of tritium in composition of two-fold labeled benzene in the presence of potassium tetrafluoroborate in the closed system. Method provides improving method of synthesis of labeled benzene and to use ion-molecular reaction of tritium-labeled phenyl cations for simultaneous, simple and a single-step synthesis of N-phenylpicolinium salts and phenyl-substituted picolines labeled with tritium that can be used in investigations of metabolism of biologically active heterocyclic derivatives.;EFFECT: improved method of synthesis.;1 dwg, 1 ex
机译:技术领域本发明涉及一种制备具有通式[CH 3 C <的苯环的labeled标记的N-苯基吡啶啉盐和苯基取代的甲基吡啶的方法。 Sub> 5 H 4 N + C 6 H * &hairsp; 5 < / Sub>] BF -&hairsp; 4 和CH 3 C 6 H * &hairsp; 5 C 5 H 3 N。该方法涉及在封闭的系统中,在四氟硼酸钾的存在下,在2-标记的苯的组成中,将beta,β-pic和2-吡啶啉与由in的β-衰变获得的游离苯基阳离子芳基化。该方法提供了标记苯的合成的改进方法,并利用of标记的苯基阳离子的离子分子反应同时,简单,一步合成了N标记的N-苯基吡啶啉盐和苯基取代的甲基吡啶,可用于生物活性杂环衍生物的代谢研究。效果:改进的合成方法; 1 dwg,1 ex

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