88285-82-9Relevant academic research and scientific papers
Synthesis of multifunctionalized phosphonic acid esters via opening of oxiranes and azetidinium salts with phosphoryl-substituted carbanions
Bakalarz-Jeziorna,Helinski,Krawiecka
, p. 1086 - 1090 (2001)
Ring-opening of N,N-diethyl-3-benzyloxyazetidinium salt 1b and N,N-dibenzyl-2,3-epoxypropylamine 6 by phosphoryl-substituted carbanions generated from phosphonates 2a-e furnishes the multifunctional phosphonates 3a-e and 7a, 7b, 7e bearing the same carbon skeleton. The reaction of the heterocyclic electrophiles 1b and 6 with the P-allyl anion generated from 2f demonstrates the strong dependence of the α/γ-regioselectivity on the reaction conditions. Depending on the character of the electrophile and/or the reaction medium the regioselective synthesis of both a α- and γ-regioisomers is realized.
Amino functional poly(ethylene glycol) copolymers via protected amino glycidol
Obermeier, Boris,Wurm, Frederik,Frey, Holger
, p. 2244 - 2251 (2010)
The synthesis of poly (ethylene glycol) (PEG) copolymers with multiple amino functionalities within the chain is described, relying on an epoxide comonomer bearing a protected amino group. N,Ndibenzyl amino glycidol (DBAG) and ethylene oxide (EO) were copolymerized via anionic polymerization, leading to well-defined polymers with varied comonomer content and low polydispersities (Mw/Mn in the range of 1.1 to 1.2). Subsequent hydrogenolysis with Pearlman's catalyst afforded polyethylene glycol-coamino glycerols (PEG-coPAG) with a precisely adjusted number of randomly incorporated amino groups in the range of 2-15%. For the first time, the kinetics of an. EO copolymerizations have has been directly monitored by 1H NMR spectroscopy in real time. Monomer consumption and compositional drift in monomer feed have been studied for various reaction temperatures, revealing a slightly tapered yet random DBAG distribution in the copolymers. The random structure of the copolymers was confirmed by detailed 13C NMR characterization of EO- and DBAG-centered triad sequence distribution and DSC measurements.
Regio- And Diastereoselective Synthesis of 2-Arylazetidines: Quantum Chemical Explanation of Baldwin's Rules for the Ring-Formation Reactions of Oxiranes ?
Kovács, Ervin,Faigl, Ferenc,Mucsi, Zoltán
, p. 11226 - 11239 (2020/10/12)
A general, scalable two-step regio- and diastereoselective method has been described for the synthesis of versatile alkaloid-type azetidines from simple building blocks with excellent overall yields. In the kinetically controlled reaction, only the format
CHEMICAL COMPOUNDS
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Page/Page column 22, (2013/07/05)
Compounds according to formula (I) or formula (II) wherein R1 and R2, independently from each other, are chosen among hydrocarbons having from 1 carbon atom up to 30 carbon atoms, with the proviso that at least one of R1 and R2 are chosen among hydrocarbons having at least 8 carbon atoms, and A is a halogen. Use of compounds as hydrophobing agent, such as sizing agent.
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors
Kumar, Arun Babu,Anderson, Jordan Micheal,Melendez, Anthony Lester,Manetsch, Roman
supporting information; experimental part, p. 4740 - 4744 (2012/08/07)
A library of 1,3-disubstituted 2-propanols was synthesized and evaluated as low molecular weight probes for β-secretase inhibition. By screening a library of 121 1,3-disubstituted 2-propanol derivatives, we identified few compounds inhibiting the enzyme at low micromolar concentrations. The initial hits were optimized to yield a potent BACE-1 inhibitor exhibiting an IC 50 constant in the nanomolar range. Exploration of the pharmacological properties revealed that these small molecular inhibitors possessed a high selectivity over cathepsin D and desirable physicochemical properties beneficial to cross the blood-brain barrier.
Synthesis of α-aliphatic and β-aromatic substituted taurines via regioselective ring opening of thiiranes with ammonia
Yu, Hao,Cao, Shengli,Zhang, Leilei,Liu, Gang,Xu, Jiaxi
experimental part, p. 2205 - 2209 (2010/02/27)
Thiiranes are important starting materials for the synthesis of substituted taurines. The regioselectivity of ring-opening reactions of thiiranes with ammonia in the presence of silver nitrate was investigated. The results of the ring-opening reaction and subsequent peroxy acid oxidation indicate that alkyl-substituted thiiranes give rise to 1-monoalkyl- and 1,1-dialkyltaurines, whereas aryl-substituted thiiranes produce 2-aryl-, 2-alkyl-2-aryl-, and 2,2-diaryltaurines. This shows that alkyl-substituted thiiranes were attacked on their less-substituted ring carbon atoms, while aryl-substituted thiiranes were attacked on their more substituted ring carbon atoms. The current method is an effective and atom-economic route for the synthesis of mono- and disubstituted α-alkyl-and β-aryl-substituted taurines. Georg Thieme Verlag Stuttgart.
TRIMERIC MACROCYCLICALLY SUBSTITUTED BENZENE DERIVATIVES
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Page 37; 38, (2010/02/08)
The invention relates to the metal complexes of general formula (I), wherein Hal represents bromine or iodine, and A1 and A2 have different meanings. The inventive metal complexes are suitable for use as contrast media.
Trimeric macrocyclic substituted benzene derivatives
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Page/Page column 13, (2010/02/10)
The metal complexes of general formula I in which Hal stands for bromine or iodine and A1 and A2 have different meanings, are suitable as contrast media.
Macrocyclic polymer complexing agents, their complexes, process for their production and pharmaceutical agents containing these compounds
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, (2008/06/13)
Polymeric compounds of general formula I in which M stands for the radical of a macrocyclic complexing agent, A stands for a backbone molecule, which shows a deficit of n amino groups, n hydroxy groups or n carboxy groups, n stands for the numbers 1 to 40
DIAMINE DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS
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, (2008/06/13)
Diamine derivatives corresponding to the general formula I EQU1 which have a highly selective action on histamine-H 2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds an
