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ISSN 0012-5008, Doklady Chemistry, 2019, Vol. 487, Part 1, pp. 173–176. © Pleiades Publishing, Ltd., 2019. Russian Text © The Author(s), 2019, published in Doklady Akademii Nauk, 2019, Vol. 487, No. 1. CHEMISTRY a, a a a V. P. Shevchenko *, L. A. Andreeva , I. Yu. Nagaev , and Academician N. F. Myasoedov Received December 5, 2018 Abstract—The synthesis of Boc-Gly-Pro-Dox, Boc-Gly-Pro-DOPA, and Boc-Gly-Pro-Srt and their deu- terated analogues was carried out. The condensation is accompanied by side reactions, which could be min- imized by optimizing the reaction conditions. The most versatile approach to the synthesis of Boc-Gly-Pro- Dox, Boc-Gly-Pro-DOPA, and Boc-Gly-Pro-Srt and their deuterated analogues is condensation of Boc- Gly-Pro or Boc-Gly-[ H]Pro with the amino groups of dopamine, serotonin, and doxorubicin. For the introduction of hydrogen isotopes into ΔPro, hydrogenation of its aqueous solution followed by condensation of the reduced proline with Boc-GlyOSu is recommended. Mass spectrometry was used to determine the content of isotopomers in the deuterated products. DOI: 10.1134/S00125008190700 48 The targeted delivery of a biologically active sub- Gly-Pro-Dox), dopamine (Boc-Gly-Pro-DOPA), stance (drug) to a particular organ, i.e., directly to and serotonin (Boc-Gly-Pro-Srt), which play the body tissue to be treated, is a challenge.
Doklady Chemistry – Springer Journals
Published: Aug 12, 2019
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