- Interchangeable PEG-supported synthesis of peptide-oligonucleotide chimeras
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A procedure has been developed for the preparation of peptide-PEG- oligonucleotide conjugates: the two sequences were synthesized at the extremities of the same commercial high-molecular-weight polyethylene glycol (PEG) starting both from the peptide as well as from the oligonucleotide component. The commercial PEG was modified at its terminal hydroxyl functions with two orthogonal protecting groups (DMT and Fmoc). The selective removal of those groups allowed the synthesis of the chimeras following two different, interchangeable strategies. Comparison of the final conjugates suggested that their production was equally effective. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Adamo, Ilaria,Ballico, Maurizio,Campaner, Pietro,Drioli, Sara,Bonora, Gian Maria
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- Recycling the versatile pipecolic linker
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The Pipecolic linker is a new highly versatile handle which immobilizes on solid support through a carboxylic acid function a wide range of amines, alcohols, and hydrazines. The anchoring step on pipecolic resin is very easy and efficient, and compounds are released with high purities upon acidic treatment. During this treatment, an oxazolonium intermediate is hydrolyzed, yielding the cleavage of ester or amide bond and the release of free carboxylic acid of the starting linker. In this study, we report the possibility of recycling the pipecolic resin after the use of several trifluoroacetic acid (TFA) cleavage cocktails. We demonstrate that it can be reused up to five times without significant loading decrease.
- Zajdel, Pawel,Masurier, Nicolas,Sanchez, Pierre,Pawlowski, MacIej,Kreiter, Aude,Nomezine, Gael,Enjalbal, Christine,Amblard, Muriel,Martinez, Jean,Subra, Gilles
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- Degradable hydrogel under physiological conditions
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The present invention discloses a hydrogel that can be degraded under physiological conditions. The hydrogel includes at least one backbone moiety and an optional crosslinking moiety, and biodegradable linkers connecting backbone moieties and crosslinking moieties can be degraded by intramolecular cyclization.
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Paragraph 0410; 0412
(2020/09/09)
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- BIOREVERSABLE PROMOIETIES FOR NITROGEN-CONTAINING AND HYDROXYL-CONTAINING DRUGS
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Disclosed are promoieties of the following formula which can be used to form prodrugs of nitrogen-containing or hydroxyl-containing drug or a pharmaceutically active agent: (I) and pharmaceutical compositions comprising the prodrugs.
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Page/Page column 136
(2015/06/18)
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- Flow-mediated synthesis of Boc, Fmoc, and Dd iv monoprotected diamines
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A series of monoprotected aliphatic diamines (21 examples) were synthesized via continuous flow methods. The carbamates and enamines were obtained in 45-91% yields using a 0.5 mm diameter PTFE tubular flow reactor. Using readily accessible protecting group precursors, the procedure serves as an attractive alternative to existing batch-mode synthetic routes by providing direct, multigram access to N-Boc-, N-Fmoc-, and N-Ddiv-protected compounds with productivity indexes of 1.2-3.6 g/h.
- Jong, Thingsoon,Bradley, Mark
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supporting information
p. 422 - 425
(2015/03/03)
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