209115-32-2Relevant academic research and scientific papers
PHARMACEUTICAL COMPOSITION FOR RESPIRATORY ADMINISTRATION
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Paragraph 0261, (2016/06/28)
The present invention provides a pharmaceutical composition for respiratory administration containing a polysaccharide derivative having a group derived from a polysaccharide and a group derived from a physiologically active substance that is covalently b
A facile synthesis of ω-aminoalkyl ammonium hydrogen phosphates
Kong, Wei Bo,Zhou, Xiao Yong,Yang, Yang,Xie, Xing Yi
experimental part, p. 923 - 926 (2012/09/21)
A series of ω-aminoalkyl ammonium hydrogen phosphates were synthesized through a simple and efficient three-step method. The starting materials, ω-aminoalkyl alcohols (AC-n, with carbon number n = 3, 4, 5, 6), were amino-protected with 9-fluorenylmethyl chloroformate (Fmoc-Cl), followed by phosphorylation with POCl3 and deprotection in piperidine/DMF. The structures of each intermediate and final product were confirmed by 1H NMR, FTIR and mass spectrum. The yield of each step was about 77-92%, with a total yield higher than 56%. This new method was superior in low-cost raw materials, mild reaction temperatures (0-25°C) and easy purification methods.
A versatile annulation protocol toward novel constrained phosphinic peptidomimetics
Nasopoulou, Magdalini,Georgiadis, Dimitris,Matziari, Magdalini,Dive, Vincent,Yiotakis, Athanasios
, p. 7222 - 7228 (2008/02/12)
(Chemical Equation Presented) The development of a novel 3-center 2-component annulation reaction between α,ω-carbamoylaldehydes and suitably monoalkylated phosphinic acids is reported. Depending on the starting α,ω-carbamoylaldehyde, diverse phosphinic scaffolds varying in the size of their rigidity element, the nature and stereochemistry of substituents, and the participation of heteroatoms in the azacyclic ring system can be obtained in one synthetic step and in high yield. In addition, this methodology allows the synthesis of Fmoc-protected constrained aminophosphinic acids that can be easily converted to suitable pseudodipeptide building blocks compatible with the requirements of peptide synthesis on the solid phase. Finally, the careful choice of both substituents and protecting groups can provide functionally diverse, orthogonally protected constrained scaffolds for extended derivatization of the target phosphinic peptidomimetic structrures.
Mycosamine orientation of amphotericin B controlling interaction with ergosterol: Sterol-dependent activity of conformation-restricted derivatives with an amino-carbonyl bridge
Matsumori, Nobuaki,Sawada, Yuri,Murata, Michio
, p. 10667 - 10675 (2007/10/03)
Amphotericin B (AmB 1) is known to assemble together and form an ion channel across biomembranes. The antibiotic consists of mycosamine and macrolactone moieties, whose relative geometry is speculated to be determinant for the drug's channel activity and
New nonnucleoside substrates for terminal deoxynucleotidyl transferase: Synthesis and dependence of substrate properties on structure
Khandazhinskaya,Kukhanova,Jasko
, p. 352 - 356 (2008/02/03)
N-(9-Fluorenylmethoxycarbonyl)-ω-aminoalkyl-, N-(9- fluorenylmethoxycarbonyl)-8-amino-3,6-dioxaoctyl, and N-[(9- fluorenylmethoxycarbonyl)-6-aminohexanoyl]-2-aminoethyl triphosphates were synthesized. All of them were shown to be the substrates of the cal
The Synthesis of Oxa-Analogues and Homologues of Naturally Occuring Polyamines
Lin, P. Kong Thoo,Kuksa, V. A.,Maguire, N. M.
, p. 859 - 866 (2007/10/03)
A number of polyamine oxa-analogues 14a-d, 19 have been synthesized.Spermidine oxa-analogues and homologues 14 were made from N-(aminooxypropyl)phthalimide 8a which was obtained either from the Fmoc-deprotection of N-phthalimide 4a or from the reaction between 3-bromopropylamine and N-hydroxyphthalimide, both reactions involving an unusual rearrangement mechanism.Sulphonated derivatives 9, 16, upon Mitsunobu condensation with N-protected 3-aminopropanol or N-alkylation with N-(bromoalkyl)phthalimides, afforded the fully protected spermidine and spermine oxa-analogues.Subsequent sequential deprotection gave spermidine analogues 14.Using the same strategy, spermine oxa-analogues 19 was synthesised. - Keywords: polyamines; oxa-analogues of polyamines; polyamine homologues; rearrangement; synthesis
