2432-03-3Relevant articles and documents
Heterobifunctional Rotaxanes for Asymmetric Catalysis
Daniliuc, Constantin G.,Grimme, Stefan,Huber, Alexander,Jansen, Dennis,Niemeyer, Jochen,Pairault, No?l,Zhu, Hui
, p. 5102 - 5107 (2020)
Heterobifunctional rotaxanes serve as efficient catalysts for the addition of malonates to Michael acceptors. We report a series of four different heterobifunctional rotaxanes, featuring an amine-based thread and a chiral 1,1′-binaphthyl-phosphoric-acid-b
The Effect of SiMe3 and SiEt3 Para Substituents for High Activity and Introduction of a Hydroxy Group in Ethylene Copolymerization Catalyzed by Phenoxide-Modified Half-Titanocenes
Kitphaitun, Suphitchaya,Nomura, Kotohiro,Yan, Qing
supporting information, p. 23072 - 23076 (2020/10/12)
Remarkable effects of SiMe3 and SiEt3 para-substituents in the phenoxide-modified half-titanocenes, Cp*TiCl2(O-2,6-iPr2-4-R-C6H2) [R=SiMe3 (6), SiEt3 (7)],
GABAA Receptor allosteric enhancement compounds and their preparation and use
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Paragraph 0054-0060, (2020/03/17)
A GABA A receptor allosteric enhancer compound and preparation and a use thereof are disclosed. The compound has a structure represented by formula (1). R 1 and R 2 are each independently selected from isopropyl and n-propyl; and when R 1 is n-propyl, R 2 is not isopropyl.
Regioselective bromination of arenes mediated by triphosgene-oxidized bromide
Xu, Yingzhou,Hu, Dufen,Zheng, Hui,Mei, David,Gao, Zhaobo
supporting information, (2019/08/30)
This article first time describes triphosgene (BTC) as an oxidant while the non-toxic and easy-to-handle potassium bromide (KBr) as the source of bromine to the bromination reaction of aromatic substrates. The novel brominating protocol gives excellent para-regioselectivity of the alkoxyl/hydroxyl arenes and high yield, offering good potential of commercial scale applications. The mechanism of “Triphosgene oxidize bromide” was proposed.
Activation and modulation of recombinant glycine and GABAAreceptors by 4-halogenated analogues of propofol
Germann, Allison L,Shin, Daniel J,Manion, Brad D,Edge, Christopher J,Smith, Edward H,Franks, Nicholas P,Evers, Alex S,Akk, Gustav
, p. 3110 - 3120 (2016/11/24)
Background and Purpose: Glycine receptors are important players in pain perception and movement disorders and therefore important therapeutic targets. Glycine receptors can be modulated by the intravenous anaesthetic propofol (2,6-diisopropylphenol). Howe
Role of steric hindrance in the Newman-Kwart rearrangement and in the synthesis and photophysical properties of arylsulfanyl tetrapyrazinoporphyrazines
Novakova, Veronika,Miletin, Miroslav,Filandrova, Tereza,Lenco, Juraj,Ruiszicka, Ales,Zimcik, Petr
, p. 2082 - 2093 (2014/04/03)
Conditions for the Newman-Kwart rearrangement of phenols into thiophenols were investigated in relation to the bulkiness of substituents at the 2 and 6 positions of the starting phenol derivative with an emphasis on eliminating side reactions. Thiophenols with different 2,6-disubstitution patterns (including hydrogen, methyl, isopropyl or tert-butyl groups) were used for the synthesis of 5,6-bis(arylsulfanyl)pyrazine-2,3-dicarbonitriles that underwent cyclotetramerization leading to the corresponding zinc tetrapyrazinoporphyrazines (TPyzPz), aza-analogues of phthalocyanines. Several methods for the cyclotetramerization were attempted to eliminate problematic side reactions. Magnesium butoxide was found as the most suitable cyclotetramerization agent and afforded TPyzPzs in reasonable yields of approximately 30% under mild conditions. The varying arrangements of the peripheral substitutions resulting from the different bulkiness of the substituents were demonstrated by the X-ray structures of the pyrazine-2,3-dicarbonitriles. The prepared zinc arylsulfanyl TPyzPzs showed an absorption maximum at a Q-band over 650 nm, fluorescence quantum yields between 0.078 and 0.20, and singlet oxygen quantum yields ranging 0.58-0.69. TPyzPzs with isopropyl groups were found to be the best derivatives in this series as they combined facile cyclotetramerization, no aggregation, and good photophysical properties, which makes them potentially suitable for photodynamic therapy.
COMPOUNDS FOR USE IN THE TREATMENT OF PAIN
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Page/Page column 20, (2010/07/02)
The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
Comparative molecular field analysis and synthetic validation of a hydroxyamide-propofol binding and functional block of neuronal voltage-dependent sodium channels
Brown, Milton L.,Eidam, Hilary A.,Paige, Mikell,Jones, Paulianda J.,Patel, Manoj K.
scheme or table, p. 7056 - 7063 (2009/12/24)
Voltage gated sodium channels represent an important therapeutic target for a number of neurological disorders including epilepsy. Unfortunately, medicinal chemistry strategies for discovering new classes of antagonist for trans-membrane ion channels have
Discovery of novel soluble crystalline anesthetics
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Page/Page column 9, (2010/11/25)
The invention discloses compounds derived from propofal which have greater aqueous solubility than propofal and are useful as anesthetic agents. The invention further discloses methods of preparing compounds of the invention. The invention also discloses
Studies towards the biomimetic synthesis of pyridomacrolidin
Irlapati, Nageswara Rao,Baldwin, Jack E.,Adlington, Robert M.,Pritchard, Gareth J.,Cowley, Andrew R.
, p. 4603 - 4614 (2007/10/03)
A possible biomimetic synthesis of pyridomacrolidin has been proposed and experimentally supported by carrying out a model study. Regio and stereospecific [3+2] cycloaddition of an in situ generated unusual di-tert-butylated acyl nitrone with Z-2-cyclodecenone and subsequent aromatisation was the key step in our proposed biomimetic synthesis. Finally a pyridomacrolidin analogue was prepared via Friedel-Crafts di-de-t-butylation of the cycloadduct.
