A simple and convenient synthesis of ω-iodoaliphatic carboxylic acids and esters by the reaction of cyclic ketones with iodine and hydrogen peroxide in the presence of catalytic CuCl has been developed. ω-Iodoaliphatic carboxylic esters were further used for the efficient preparation of di(2-pyridylmethylamino)alkanoic acids in excellent yields.
В настоящее время проводятся доклинические исследования нового производного октреотида с хелатный центром (DPAH-октреотид) для связывания 99mTc, для радионуклидной диагностики нейроэндокринных опухолей. Способ получения DPAH-октреотида основан на реакции образования амидной связи между амино-группой остатка D-фенилаланина и бифункциональным хелатирующим агентом сукцинимид-1-ил 6-(бис(пиридин-2-илметил)амино)гексаноатом. Для обеспечения качества DPAH-октреотида предложена ВЭЖХ методика для определения подлинности, посторонних примесей и количественного содержания. При проведении валидации установлено, что по параметрам — специфичность, предел обнаружения, линейность, правильность, сходимость и внутрилабораторная прецизионность аналитическая методика ВЭЖХ определения показателей качества DPAH-октреотида соответствует требованиям, предъявляемым к методикам, и может использоваться для контроля качества готовой продукции при производстве реагента для приготовления радиофармацевтического препарата на его основе.
Currently the development of technologies for labeling somatostatin with technetium-99m for diagnosing radionuclide neuroendocrine tumors is under way. Somatostatin analogues are binded with technetium99m only by the preliminary addition of a chelating agent. Therefore, it is important to develop a method for preparation of an octreotide derivative by modifying octreotide with precursors: ligands with high chelating ability for its tight binding with technetium-99m. ω-Bis(pyridin-2-ylmethyl)amino)aliphatic acids can be used successfully as such precursors.The purpose of the study was to develop a method for obtaining a new octreotide derivative for diagnosing neuroendocrine tumors.Materials and methods. The somatostatin octreotide analogue was used as the object of the study; succinimid-1-yl 6-(bis(pyridin-2-ylmethyl)amino)hexanoate was used as a chelating agent. Methods of high performance liquid chromatography and mass spectrometry were used to separate and analyze the synthesized compounds.Results. A method to produce an original octreotide derivative using a succinimid-1-yl 6-(bis(pyridin2-ylmethyl)amino)hexanoate as a chelating agent was proposed. The conditions of analytical and semipreparative HPLC for the analysis and purification of the active octreotide derivative (a monosubstituted derivative of the amino acid residue of D-phenylalanine) were suggested.Conclusion. The synthesized derivative of octreotide has a chelating center for strong binding to technetium-99m in its structure, which can be useful for diagnosing neuroendocrine tumors.
The arylation of azaheterocycles can be considered as one of the most important processes for the preparation of various biologically active compounds. In the present work, we describe a method...
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