chemicallytechFine Chemical TechnologiesТонкие химические технологии2410-65932686-7575MIREA – Russian Technological University (RTU MIREA).chemicallytech-523Research ArticleArticlesСтатьиSynthesis of folate lipoconjugates with hydrophobic spacersСИНТЕЗ ФОЛАТСОДЕРЖАЩИХ ЛИПОКОНЪЮГАТОВ С ГИДРОФОБНЫМИ СПЕЙСЕРНЫМИ ГРУППАМИШмендельЕ. В.ShmendelE. V.noemail@neicon.ruЕреминС. В.EreminS. V.noemail@neicon.ruМорозоваН. Г.MorozovaN. G.noemail@neicon.ruМасловМ. А.MaslovM. A.mamaslov@mail.ruМосковский государственный университет тонких химических технологий им. М.В. ЛомоносоваРоссияM.V. Lomonosov Moscow State University of Fine Chemical Technologies, 86, Vernadskogo pr., Moscow 119571Russian FederationМосковский государственный университет тонких химических технологий им. М.В. ЛомоносоваRussian Federation20132812201386111113Copyright © Shmendel E.V., Eremin S.V., Morozova N.G., Maslov M.A., 20132013Шмендель Е.В., Еремин С.В., Морозова Н.Г., Маслов М.А.Shmendel E.V., Eremin S.V., Morozova N.G., Maslov M.A.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.finechem-mirea.ru/jour/article/view/523

Folate lipoconjugates were synthesized by induction of spacers to 1,2-di-O-tetradecyl-rac-glycerol for future condensation with folic acid. The intermediates hydrophobic compounds were obtained by treatment of 1-О-(4- nitrophenyloxycarbonyl)-2,3-di-O-tetradecyl-rac-glycerol with free diamines (1,4-diaminobutane, 1,6-diaminohexane, 1,8-diaminooctane, 1,12-diaminododecane) in the presence of triethylamine. Condensation of intermediate compounds (1 eq.) and folic acid (3 eq.) were carried out in the presence of (O-(benzotriazol-1-yl)- 1,1,3,3-tetramethyluronium tetrafluoroborate (3 eq.) and N,N-diisopropylethylamine (5 eq.) and gave targeted folate lipoconjugates. The structures and purity of the compounds synthesized were confirmed by analytic physicochemical methods.

П редставлен синтез фолатсодержащих липоконъюгатов, предназначенных для включения в липосомальные системы доставки противоопухолевых препаратов с целью придания им направленности на опухолевые клетки. Целевые соединения амфифильной природы выделены по разработанной оригинальной методике.

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The authors declare that there are no conflicts of interest present.