Synthesis of folate lipoconjugates with hydrophobic spacers
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-d...
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| Main Authors: | , , , |
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| Format: | Article |
| Language: | Russian |
| Published: |
MIREA - Russian Technological University
2013-12-01
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| Series: | Тонкие химические технологии |
| Subjects: | |
| Online Access: | https://www.finechem-mirea.ru/jour/article/view/523 |
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| Summary: | 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. |
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| ISSN: | 2410-6593 2686-7575 |