173724-95-3Relevant articles and documents
Preparation method of chiral 3-substituted pyrrolidine derivative
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Paragraph 0064-0067, (2020/11/01)
The invention provides a preparation method of a chiral 3-substituted pyrrolidine derivative. The preparation method comprises an intermediate preparation step, a diastereomer mixture preparation step, a chiral separation step and a chiral 3-substituted pyrrolidine derivative synthesis step. According to the invention, through catalytic asymmetric kinetic resolution, a mixture of two diastereoisomers is efficiently converted into a diastereoisomer with a certain single configuration, chiral separation is realized, a key intermediate is obtained with high yield, and a series of chiral 3-substituted pyrrolidine derivatives are synthesized. The whole reaction route is mild in reaction condition, simple and convenient to operate, high in resolution efficiency, high in atom economy, low in costand suitable for industrial scale production.
Transition-metal-free synthesis of 3-(1-pyrrolidinyl)quinolines and 3-(1-pyrrolidinyl)quinoline 1-oxides via a one-pot reaction of 3-(1-pyrrolidinyl)crotonates with nitrobenzenes
Bujok, Robert,Cmoch, Piotr,Wróbel, Zbigniew,Wojciechowski, Krzysztof
supporting information, p. 2397 - 2402 (2017/03/20)
A carbanion of tert-butyl 3-(1-pyrrolidinyl)crotonate adds to nitrobenzenes to form σH-adducts, which in the presence of pivaloyl chloride and triethylamine are converted into 3-(1-pyrrolidinyl)quinolines or 3-(1-pyrrolidinyl)quinoline 1-oxides depending on the nitrobenzene structure. This is the first methodology in which a quinoline ring is constructed from a substrate bearing a pyrrolidinyl ring. Starting from optically pure enamines, the method allows synthesis of the corresponding chiral products without racemisation.
Preparation of novel azabicyclic amines and α7 nicotinic acetylcholine receptor activity of derived aryl amides
Walker, Daniel P.,Acker, Brad A.,Jacobsen, E. Jon,Wishka, Donn G.
, p. 247 - 257 (2008/09/18)
(Chemical Equation Presented) Three new azabicyclic amines, namely exo-3-amino-1-azabicyclo[3.2.1]octane, 3-amino-1-azabicyclo-[3.2.2]nonane and exo-6-amino-8-azabicyclo[3.2.1]octane, have been designed and prepared as isosteres of 3-aminoquinuclidine. Ar
SPIRO CONDENSED PIPERIDNES AS MODULATORS OF MUSCARINIC RECEPTORS
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Page/Page column 50-51, (2008/06/13)
The present invention relates to modulators of muscarnic receptors of formula (I). The present invention also provides impositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
QUINOLONE ANTIBACTERIAL AGENTS
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Page/Page column 88; 89; 122, (2010/02/12)
Compounds of formula (I) wherein A is formula (II), formula (III) or formula (IV), and B is formula (V), formula (VI), or formula (VII), can be used in a variety of applications including use as antibacterial agents.
ANTIBACTERIAL AMINOQUINAZOLIDINEDIONE DERIVATIVES
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Page/Page column 116; 117; 150, (2010/02/12)
Compounds of formula (I) wherein: A is Formula (II), Formula (III), or Formula (IV) and B is Formula (V), Formula (VI), or Formula (VII), can be used in a variety of applications including use as antibacterial agents.
1H-PYRAZOLE AND 1H-PYRROLE-AZABICYCLIC COMPOUNDS WITH ALFA-7 NACHR ACTIVITY
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Page 79-80, (2010/02/06)
The invention provides compounds of Formula (I), wherein Azabicyclo is Formula (I, II, III, IV, V, VI, VII); W is Formula (m); where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which α7 is known to be involved.
COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES
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Page 48 - 49, (2010/02/06)
The invention discloses compounds that are selective α7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.
COMPOUNDS AS RADIOLIGANDS FOR THE DIAGNOSIS OF DISEASE
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Page 49-50, (2010/02/07)
Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11C, 18F, 76Br, 123I or 125I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon to emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.
Substituted-aryl compounds for treatment of disease
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, (2011/05/18)
The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.