946-94-1Relevant academic research and scientific papers
Glucokinase activator containing nitroquinoline structure and application thereof
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Paragraph 0034; 0037; 0038, (2017/07/19)
The invention relates to the field of medicine relevant to type II diabetes, in particular to a glucokinase activator containing a nitroquinoline structure, a preparation method of the glucokinase activator and application of the glucokinase activator to preparation of medicine for treating the type II diabetes. The structural formula of the glucokinase activator is shown in the description.
Glucokinase activating agent containing halogenated quinoline structure, preparation method and application thereof
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Paragraph 0038; 0041-0042, (2017/08/29)
The invention relates to the field of medicines related to II-type diabetes, particularly relates to a glucokinase activating agent containing a halogenated quinoline structure, a preparation method and an application thereof in preparation of II-type diabetes medicines. The structure formula is shown in the specification, wherein, X is selected from a halogen substituent group.
COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES
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Page/Page column 171; 172, (2016/06/14)
This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
A new ferrocene-based bulky pyridine as an efficient reusable homogeneous catalyst
Kashyap, Bishwapran,Phukan, Prodeep
, p. 15327 - 15336 (2013/09/02)
An effective approach to reusing a homogeneous catalyst has been demonstrated. A ferrocene-based bulky pyridine has been synthesized and utilized as a homogeneous catalyst for the synthesis of benzoylfumarates as well as for acetylation. After the reaction, the catalyst was separated by simple precipitation and reused without appreciable loss of activity. The Royal Society of Chemistry 2013.
Efficient Cu-catalyzed base-free C-S coupling under conventional and microwave heating. A simple access to S-heterocycles and sulfides
Soria-Castro, Silvia M.,Penenory, Alicia B.
supporting information, p. 467 - 475 (2013/05/08)
S-aryl thioacetates can be prepared by reaction of inexpensive potassium thioacetate with both electron-rich and electron-poor aryl iodides under a base-free copper/ligand catalytic system. CuI as copper source affords S-aryl thioacetates in good to excellent yields, by using 1,10-phenanthroline as a ligand in toluene at 100°C after 24 h. Under microwave irradiation the time was drastically reduced to 2 h. Both procedures are simple and involve a low-cost catalytic system. This methodology was also applied to the "one-pot" synthesis of target heterocycles, such as 3H-benzo[c][1,2]dithiol-3-one and 2-methylbenzothiazole, alkyl aryl sulfides, diaryl disulfides and asymmetric diaryl sulfides in good yields.
A simple, base-free preparation of S-aryl thioacetates as surrogates for aryl thiols
Van Den Hoogenband, Adri,Lange, Jos H. M.,Bronger, Raymond P. J.,Stoit, Axel R.,Terpstra, Jan Willem
experimental part, p. 6877 - 6881 (2011/03/18)
A mild method for the preparation of S-aryl thioacetates by hetero cross-coupling reactions of aryl bromides or aryl triflates with potassium thioacetate is described. The reaction proceeded smoothly in toluene at 110°C, mediated by catalytic Pd2(dba)3 in combination with CyPF-tBu as the ligand. Neither the presence of a base nor microwave conditions were required. The formed S-aryl thioacetate proved to be stable under flash chromatographic conditions and could be rapidly converted into the corresponding thiol under mildly basic conditions.
Thiocarbamates and their derivatives
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, (2008/06/13)
A process is provided for preparing N-acyl-aminothiophenols, e.g., N-acetyl-para-aminothiophenol, or aminothiophenols, e.g., para-aminothiophenol, by reacting a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone (4-HAP), with hydroxylamine or a hydroxylamine salt, to form the oxime of the ketone, subjecting the oxime to a Beckmann rearrangement in the presence of a catalyst to form the N-acyl-hydroxy aromatic amine, e.g., N-acetyl-para-aminophenol (APAP), reacting the N-acyl-hydroxy aromatic amine with an N,N-di (organo) thiocarbamoyl halide, e.g., N,N-dimethylthiocarbamoyl chloride, to form an O-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate, e.g., O-(N-acetyl-para-aminophenyl)-N,N-dimethylthiocarbamate, pyrolytically rearranging the O-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate to form an S-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate, e.g., S-(N-acetyl-para-aminophenyl)-N,N-dimethylthiocarbamate, and hydrolyzing the latter compound to obtain the N-acyl aminothiophenol or aminothiophenol. The N-acyl aminothiophenol may be reacted with an acylating agent to form the N,S-diacyl-aminothiophenol, e.g., N,S-diacetyl-p-aminothiophenol, or may be further hydrolyzed to the aminothiophenol, e.g., p-aminothiophenol.
