112523-78-1Relevant articles and documents
A flupirtin derivative and its inorganic acid salt preparation method (by machine translation)
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Paragraph 0052-0054; 0057-0058; 0065; 0068-0069; 0076, (2019/10/22)
The invention relates to a kind of flupirtine derivative and its inorganic acid salt of the preparation method, the [...] derivatives by the following chemical formula 1 that: The [...] derivative is maleic acid flupirtin synthesis process and/or storage of produced in the process of an important impurity. The preparation method according to this application, and may be the above-mentioned yield of flupirtine derivative and its inorganic acid salt, each step of the reaction yield can be up to 55% or more. (by machine translation)
Discovery of Aromatic Carbamates that Confer Neuroprotective Activity by Enhancing Autophagy and Inducing the Anti-Apoptotic Protein B-Cell Lymphoma 2 (Bcl-2)
Kinarivala, Nihar,Patel, Ronak,Boustany, Rose-Mary,Al-Ahmad, Abraham,Trippier, Paul C.
, p. 9739 - 9756 (2017/12/26)
Neurodegenerative diseases share certain pathophysiological hallmarks that represent common targets for drug discovery. In particular, dysfunction of proteostasis and the resultant apoptotic death of neurons represent common pathways for pharmacological intervention. A library of aromatic carbamate derivatives based on the clinically available drug flupirtine was synthesized to determine a structure-activity relationship for neuroprotective activity. Several derivatives were identified that possess greater protective effect in human induced pluripotent stem cell-derived neurons, protecting up to 80% of neurons against etoposide-induced apoptosis at concentrations as low as 100 nM. The developed aromatic carbamates possess physicochemical properties desirable for CNS therapeutics. The primary known mechanisms of action of the parent scaffold are not responsible for the observed neuroprotective activity. Herein, we demonstrate that neuroprotective aromatic carbamates function to increase the Bcl-2/Bax ratio to an antiapoptotic state and activate autophagy through induction of beclin 1.
A method for synthesis of flupirtine maleate
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Paragraph 0119; 0121, (2016/10/09)
The invention provides a synthesis method of flupirtine maleate. Recrystallization by use of methanol is carried out in the refining step of the crude product of the flupirtine maleate so that the product is white in appearance and high in purity, and the crystal form of the product is pure A crystal and same as the crystal form of the commercial products. The optimal reaction solvent, reaction time and reaction temperature are explored and found out by use of a simplified process flow, and a method for preparing the flupirtine maleate in the pure A crystal form, which is high in yield, low in cost and simple to operate, uses easily available raw materials and is applicable to the industrial production is found.