29681-38-7Relevant academic research and scientific papers
Asymmetric synthesis of (S)-(-)-acromelobinic acid
Adamczyk, Maciej,Akireddy, Srinivasa Rao,Reddy, Rajarathnam E.
, p. 2385 - 2387 (2001)
A total synthesis of (S)-(-)-acromelobinic acid 2, which was isolated from clitocybe acromelalga, was achieved via an asymmetric hydrogenation protocol. Dehydroamino acid derivative 12 was prepared from 2,5-lutidine 5 and subjected to asymmetric hydrogenation using (S,S)-[Rh(Et-DuPHOS)(COD)]BF4 to give the (S)-(+)-pyridylalanine derivative 13 in 93% yield and >96% e.e. Removal of the protecting groups in (S)-(+)-13 afforded (S)-(-)-acromelobinic acid 2.
Synthesis of Esters by Functionalisation of CO2
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Paragraph 0129, (2017/09/06)
The invention relates to a method for (I) producing a carboxylic ester of formula (I). Said method comprises the steps of: a) bringing an organosilane/borane of formula Si or B into contact with CO2, in the presence of a catalyst and an electrophilic compound of formula (III), the groups R1, R2, R3, R4, R5, Y, and M′ being as defined in claim 1; and optionally b) recovering the compound of formula (I) produced.
SUBSTITUTED BENZOXAZOLES
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Paragraph 1604-1605, (2016/05/10)
The invention relates to substituted benzoxazoles and to processes for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders, preferably of thrombotic or thromboembolic disorders.
Substituted benzoxazoles
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Paragraph 0509, (2016/10/10)
The invention relates to substituted benzoxazoles of formula (1) where R1 stands for a group of formula, and a method for preparing same and their use in the production of drugs for the treatment and/or prevention of diseases, in particular cardiovascular diseases, preferably thrombotic or thromboembolic diseases.
CO2 Conversion into Esters by Fluoride-Mediated Carboxylation of Organosilanes and Halide Derivatives
Frogneux, Xavier,Von Wolff, Niklas,Thuéry, Pierre,Lefèvre, Guillaume,Cantat, Thibault
, p. 2930 - 2934 (2016/03/25)
A one-step conversion of CO2 into heteroaromatic esters is presented under metal-free conditions. Using fluoride anions as promoters for the C-Si bond activation, pyridyl, furanyl, and thienyl organosilanes are successfully carboxylated with CO2 in the presence of an electrophile. The mechanism of this unprecedented reaction has been elucidated based on experimental and computational results, which show a unique catalytic influence of CO2 in the C-Si bond activation of pyridylsilanes. The methodology is applied to 18 different esters, and it has enabled the incorporation of CO2 into a polyester material for the first time. Metal free! A novel methodology is described to convert CO2 into heteroaromatic esters in the presence of organosilanes and organic halides using fluoride anions as promoters for the C-Si bond activation (see scheme). CO2 exhibits a unique catalytic influence in the C-Si bond cleavage of pyridylsilanes, serving as a traceless activator.
Development of an iron(II)-catalyzed aerobic catechol cleavage and biomimetic synthesis of betanidin
Guimond, Nicolas,Mayer, Peter,Trauner, Dirk
supporting information, p. 9519 - 9523 (2014/08/18)
An aerobic iron(II)-catalyzed cleavage of catechols was developed. This reaction allows for the preparation of 2-methoxy-2H-pyrans that can be employed as versatile building blocks for synthesis. The utility of this biomimetic oxidative cleavage is featured in the synthesis of betanidin, a natural colorant with antioxidant properties. Cut and paste: An aerobic iron(II)-catalyzed oxidative cleavage of catechol was developed. This reaction allows the preparation of 2H-pyrans that can be employed as versatile building blocks for synthesis. The utility of this biomimetic cleavage is featured in the synthesis of betanidin, the aglycone of red beets' principal colorant and itself a valuable antioxidant (see scheme).
NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0620-0621, (2013/10/22)
This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised 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 neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
NOVEL COMPOUNDS
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Page/Page column 47, (2013/06/27)
This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
NOVEL COMPOUNDS
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Paragraph 0242, (2013/06/05)
This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
AMIDO-PYRIDYL ETHER COMPOUNDS AND COMPOSITIONS AND THEIR USE AGAINST PARASITES
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Page/Page column 57, (2013/03/26)
The subject matter disclosed herein is directed to amido-pyridyl ether compounds of formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, Ra, a, b and d are as described herein, compositions comprising the compounds of formula I, methods for their preparation and methods for their uses against parasites.
