- Spermidinium closo-dodecaborate-encapsulating liposomes as efficient boron delivery vehicles for neutron capture therapy
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closo-Dodecaborate-encapsulating liposomes were developed as boron delivery vehicles for neutron capture therapy. The use of spermidinium as a counter cation of closo-dodecaborates was essential not only for the preparation of high boron content liposome solutions but also for efficient boron delivery to tumors. This journal is
- Tachikawa, Shoji,Miyoshi, Tatsuro,Koganei, Hayato,El-Zaria, Mohamed E.,Vias, Clara,Suzuki, Minoru,Ono, Koji,Nakamura, Hiroyuki
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- Synthesis process of spermidine and intermediate thereof
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The invention provides a synthesis process of spermidine (I) which takes 3 -t-butyloxycarbonyl V (N -) and -1-t-butyloxycarbonyl 4 - IV butanediamine (N -) as a raw material to obtain the spermidine trihydrochloride (-4 - II III) by reductive amination reaction, and provides a novel method for chemical synthesis of spermidine by liberation of the protecting group from the intermediate I (3 -) to obtain the spermidine (III) II.
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Paragraph 0047-0053
(2021/10/27)
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- Method for synthesizing spermidine hydrochloride
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The invention relates to a method for synthesizing spermidine hydrochloride. The reaction formula is shown as the following formula (I) which is described in the specification. In the formula (I), theprotective group R1 of amino in 4-amino-1-butanol of a compound 2 is one of tert-butyloxycarboryl Boc-, triphenylmethyl Trt- and p-methoxytriphenylmethyl Mmt-, and a protective group R2 of propane diamine of the compound is one of tert-butyloxycarbonyl Boc-, triphenylmethyl Trt- and p-methoxytriphenylmethyl (Mmt-). A reagent used in the Mitsunobo reaction condition is one of triphenylphosphine, di-tert-butyl azodicarboxylate, diethyl azodicarboxylate and diisopropyl azodicarboxylate. The preparation method disclosed by the invention is simple in required process condition, mild in reaction condition, capable of effectively obtaining spermidine hydrochloride, relatively short in synthesis step and relatively high in synthesis yield.
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Paragraph 0024-0025; 0034; 0036; 0037; 0039
(2020/07/13)
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- Synthesis of 13C-dilabeled 4-coumaroylspermidines
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Five 13C-dilabeled constitution isomers of 4-coumaroylspermidines were prepared in nine to eleven steps: N1,4-di[(E)-4-coumaroyl]-(5,8- 13C2)spermidine (13b), N1-[(E)-4-coumaroyl]-(5,8-13C2)spermidine (17b), N1,8-di[(E)-4-coumaroyl]-(1,4-13C2)spermidine (20b), N4-[(E)-4- coumaroyl]-(1,4-13C2)spermidine (24b) and N1,4,8-tri[(E)-4-coumaroyl]- (5,8-13C2)spermidine (26). The two 13C-atoms were subsequently introduced using labeled potassium cyanide. The synthesis proceeds through stepwise construction of the polyamine backbone including protection and deprotection steps of the amino functions. Based on 1H-1H NOE interactions, the preliminary study of their binding reveals that 20b binds to tRNA in the same way as spermidine does, whereas 24b and 26 do not show any NOE effects with the tRNA protons.
- Geneste, Herve,Hesse, Manfred
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p. 15199 - 15214
(2007/10/03)
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- Aliphatic Amino Azides as Key Building Blocks for Efficient Polyamine Syntheses
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New routes to open-chain polyamines have been developed using aliphatic amino azides as common precursors for the construction of the carbon-nitrogen framework.These α,ω-diaminoalkane synthetic equivalents were combined with (ω-halogenalkyl)dichloroboranes to extend the polyamine chain from the azido moiety.An extension from the free amino group can also be achieved via a Michael type addition with acrylonitrile or a reductive amination with a γ-azido ketone.Further transformations led to a large variety of regioselectively C- or (and) N-substituted polyamines.
- Carboni, Bertrand,Benalil, Aziza,Vaultier, Michel
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p. 3736 - 3741
(2007/10/02)
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- Amino protection using triazones
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Primary amines protected by incorporation into a "triazone" derivative (3) are stable to various reduction, oxidation, organometallic, and basic hydrolysis conditions, and may be regenerated by treatment with aqueous ammonium chloride at 70°. An application to polyamine synthesis is described.
- Knapp, Spencer,Hale, Jeffrey J.,Bastos, Margarita,Gibson, Frank S.
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p. 2109 - 2112
(2007/10/02)
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