26570-48-9Relevant articles and documents
A facile approach to bis(Isoxazoles), promising ligands of the ampa receptor
Averina, Elena B.,Grigoriev, Vladimir V.,Grishin, Yuri K.,Karlov, Dmitry S.,Kuznetsova, Tamara S.,Palyulin, Vladimir A.,Radchenko, Eugene V.,Rybakov, Victor B.,Sadovnikov, Kirill S.,Sedenkova, Kseniya N.,Vasilenko, Dmitry A.,Zamoyski, Vladimir L.
, (2021/11/01)
A convenient synthetic approach to novel functionalized bis(isoxazoles), the promising bivalent ligands of the AMPA receptor, was elaborated. It was based on the heterocyclization reactions of readily available electrophilic alkenes with the tetranitromethane-triethylamine complex. The structural diversity of the synthesized compounds was demonstrated. In the electrophysi-ological experiments using the patch clamp technique on Purkinje neurons, the compound 1,4-phenylenedi(methylene)bis(5-aminoisoxazole-3-carboxylate) was shown to be highly potent positive modulator of the AMPA receptor, potentiating kainate-induced currents up to 70% at 10?11 M.
Synthesis and activity of novel homodimers of Morita–Baylis–Hillman adducts against Leishmania donovani: A twin drug approach
da Silva, Wagner A.V.,Rodrigues, Daniele C.,de Oliveira, Ramon G.,Mendes, Rhuan K.S.,Olegário, Tayná R.,Rocha, Juliana C.,Keesen, Tatjana S.L.,Lima-Junior, Claudio G.,Vasconcellos, Mário L.A.A.
supporting information, p. 4523 - 4526 (2016/08/24)
It is reported here the synthesis of novel Homodimers 12–19 of Morita–Baylis–Hillman adducts (MBHA) from one-pot Morita–Baylis–Hillman Reaction (MBHR) between aromatic aldehydes as eletrophiles and ethylene glycol diacrylate as Michael acceptor (35–94% yields) using cheap and green conditions. The bioactivities were evaluated against promastigote form of Leishmania donovani. All homodimers showed to be more potent than corresponding monomers. It is worth highlighting that the halogenated homodimers 17 and 18 (0.50?μM) is almost 400 times more active than the corresponding monomer 10 and 1.24 times more potent than the second-line drug amphotericin B (0.62?μM). Moreover, the selectivity index to 18 is very high (SIrb?>?400) far better than amphotericin B (SIrb?=?18.73). This is the first report of twin drugs strategy applied on Morita–Baylis–Hillman adducts.
Method for catalytically synthesizing diethylene glycol di(methyl) acrylate by calcium glyceroxide
-
Paragraph 0041; 0042, (2017/01/02)
The invention discloses a method for catalytically synthesizing diethylene glycol di(methyl) acrylate by calcium glyceroxide, and belongs to the field of fine chemical engineering. (Methyl) alkyl acrylate and diethylene glycol are used as raw materials; a reaction-rectification coupling process is adopted; a copper-wire-net-filled modified rectification column is used; the catalyst calcium glyceroxide is added; enough product purity and yield can be obtained after a simple aftertreatment process. The method overcomes multiple disadvantages of an existing transesterification catalyst, and is high in yield and simple in post-processing. Compared with a conventional transesterification method, the method provided by the invention can improve the total yield and the processing capacity; energy needed for separation is supplied by utilizing reaction heat, so that the energy consumption is decreased, and an investment is reduced. The method provided by the invention is simple and short in process flow; the raw materials are easily obtained; equipment is simple; reaction conditions are easy to control. The method is mild in the reaction conditions and simple in purification and refining processes; a product is stable, is easy to separate, and is not liable to generate a polymerization phenomenon.
