1071435-62-5Relevant articles and documents
Asymmetric Biocatalytic Synthesis of Fluorinated Pyridines through Transesterification or Transamination: Computational Insights into the Reactivity of Transaminases
López-Iglesias, María,González-Martínez, Daniel,Rodríguez-Mata, María,Gotor, Vicente,Busto, Eduardo,Kroutil, Wolfgang,Gotor-Fernández, Vicente
, p. 279 - 291 (2017)
The synthesis of a family of pyridines bearing a fluorinated substituent on the aromatic ring has been carried out through two independent and highly stereoselective chemoenzymatic strategies. Short chemical synthetic routes toward fluorinated racemic amines and prochiral ketones have been developed, which served as substrates to explore the suitability of lipases and transaminases in asymmetric biotransformations. The lipase-catalyzed kinetic resolution via acylation of racemic amines proceeded smoothly giving conversions close to 50% and excellent enantioselectivities. Alternatively, the biotransamination of the corresponding prochiral ketones was investigated giving access to both optically pure amine enantiomers using transaminases with complementary selectivity. High to quantitative conversion values were achieved, which allowed the isolation of the amines in moderate to high yields (40–88%). A deeper understanding of the latter process was enabled by performing theoretical calculations on thermodynamic and mechanistic aspects. Calculations showed that the biotransamination reactions are highly favoured by the presence of fluorine atoms and the pyridine ring. (Figure presented.).
N-formamido pyrazoline derivative serving as P2X3 receptor antagonist and application thereof
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Paragraph 0118; 0123-0124; 0125; 0128, (2020/11/23)
The invention discloses an N-formamido pyrazoline derivative, a compound represented by a general formula (I) or an enantiomer, a diastereoisomer, an epimer, a racemate or pharmaceutically acceptablesalt thereof. The compound is an antagonist of a ligand gated non-selective cationic channel receptor subtype P2X3, and can be used for treating or preventing various diseases mediated by a P2X3 receptor.
PYRID-2-YL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSITIONS AND USES THEREOF
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, (2008/12/04)
Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
2-Cyanophenyl fused heterocyclic compounds, and compositions and uses thereof
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Page/Page column 26, (2008/12/08)
Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.