154343-02-9Relevant academic research and scientific papers
Substituted pyridine compound and its method and use thereof
-
Paragraph 0467; 0468, (2018/06/21)
The invention relates to a novel substitutive pyridine compound, and a pharmaceutically acceptable salt and a pharmaceutical preparation of the substitutive pyridine compound for regulating the activity of protein kinases and regulating signal responses between cells or in the cells. Meanwhile, the invention further relates to a pharmaceutical composition containing the compound provided by the invention, and a method for treating high proliferative diseases of mammals, especially human with the pharmaceutical composition.
Flexible synthesis of planar chiral azoninones and optically active indolizidinones
Bohland, Frank,Erlin, Irina,Platte, Lukas,Schr?der, Maike,Schollmeyer, Dieter,Nubbemeyer, Udo
supporting information, p. 6272 - 6284 (2015/03/30)
The flexible synthesis of defined substituted optically active indolizidinones starting from chiral pool (S)-proline and trans 4-hydroxy-(S)-proline is described. Several defined 2-vinylpyrrolidines were generated in short sequences. The aza-Claisen rearr
NHC-Catalyzed intramolecular redox amidation for the synthesis of functionalized lactams
Thai, Karen,Wang, Li,Dudding, Travis,Bilodeau, Francois,Gravel, Michel
supporting information; experimental part, p. 5708 - 5711 (2011/03/19)
A very efficient NHC-catalyzed lactamization reaction is reported. For most cases, the ring expansion reaction proceeds to cleanly furnish five- and six-membered N-Ts and N-Bn lactams, without the need for further purification. Evidence is presented suggesting a dual role for the stoichiometric base: (1) deprotonation of the triazolium precatalyst and (2) activation of the nitrogen leaving group through hydrogen bonding.
Highly enantioselective synthesis of β-amino alcohols: A catalytic version
Metro, Thomas-Xavier,Pardo, Domingo Gomez,Cossy, Janine
, p. 6556 - 6561 (2008/02/10)
(Chemical Equation Presented) Highly enantioselective rearrangement of β-amino alcohols was realized by using a catalytic amount of trifluoroacetic anhydride.
Enantioselective diethylzinc addition to aromatic and aliphatic aldehydes using (3R,5R)-dihydroxypiperidine derivatives catalyst
Roudeau, Rémi,Gomez Pardo, Domingo,Cossy, Janine
, p. 2388 - 2394 (2007/10/03)
A series of chiral (3R,5R)-dihydroxypiperidine derivatives 3a-f were conveniently prepared from trans-4-hydroxy-l-proline and applied to the catalytic enantioselective addition of diethylzinc to benzaldehyde and heptanal. Among them, 3d was found to show
Design and synthesis of conformationally frozen peptide nucleic acid backbone: Chiral piperidine PNA as a hexitol nucleic acid surrogate
Lonkar, Pallavi S.,Kumar, Vaijayanti A.
, p. 2147 - 2149 (2007/10/03)
The design and facile synthesis of novel chiral piperidine PNA from naturally occurring 4-hydroxy-L-proline is reported. The stereospecific ring-expansion reaction to get six-membered piperidine derivative from 5-membered pyrrolidine derivative is exploit
Enantiospecific synthesis and receptor binding of novel dopamine receptor ligands employing natural 4-hydroxyproline as a practical and flexible building block
Heindl, Cornelia,Huebner, Harald,Gmeiner, Peter
, p. 3153 - 3172 (2007/10/03)
Starting from natural 4-hydroxyproline, an ex-chiral pool approach is described giving access to 2-aminoalkylpyrrolidine derivatives that were used as chiral building blocks for the synthesis of bioactive 2-methoxybenzamide derivatives. The 4-hydroxy substituent can be displaced employing organocuprates as useful carbanion equivalents. Dopamine and serotonin binding studies involving the subtypes D1, D2long, D2short, D3 and D4 as well as 5-HT1A and 5-HT2, respectively, provided interesting insights into stereoselective structure activity relationships. The (2S,4R)-2-aminomethylpyrrolidine derivative ent-66 and the (2R,4S)-2- aminoethylpyrrolidine derivative 68 showed remarkable affinity and preference for the dopamine D3 and D4 receptor subtypes, respectively, both being putatively associated to the symptoms of schizophrenia.
Piperidinyl peptide nucleic acids: Synthesis and DNA-complementation studies
Lonkar, Pallavi,Kumar, Vaijayanti A.
, p. 1105 - 1108 (2007/10/03)
Synthesis of a new six membered PNA analogue by introducing a methylene bridge between β carbon atom of ethylene diamine and β′ carbon atom of linker to nucleobase.
Asymmetric synthesis of α-branched primary amines on solid support via novel hydrazine resins
Enders, Dieter,Kirchhoff, Jan H.,Koebberling, Johannes,Peiffer, Thomas H.
, p. 1241 - 1244 (2007/10/03)
Matrix presented Two novel chiral hydrazine resins for asymmetric solid-phase synthesis have been developed. The enantiopure β-methoxyamino auxiliaries, derived from frans-4-hydroxy-(S) -proline and (R) -leucine, were attached to Merrifield resin and transformed into their corresponding hydrazines. Immobilization of various aldehydes, followed by 1,2-addition of organolithium reagents to the resulting enantiopure hydrazones and reductive cleavage from the solid support, furnished α-branched amines, which were isolated as their corresponding amides in good overall yields and enantiomeric excesses of up to 86%.
Unusual diastereoselection in the synthesis of nine-membered ring lactams and conformation-controlled transannular reactions to generate optically active indolizidinones
Sudau, Alexander,Nubbemeyer, Udo
, p. 1140 - 1143 (2007/10/03)
The aza-Claisen rearrangement of vinylpyrrolidines 1 yielded almost exclusively the trans-3,8-disubstituted nine-membered ring lactams 2 (TBS = tBuMe2Si), independent of whether cis or trans isomers were used as starting materials. The conforma
