75510-02-0Relevant academic research and scientific papers
Application of Cu-MOF (Metal Organic Framework) type catalyst in preparing polysubstitution pyridine derivative
-
Paragraph 0126; 0127; 0128; 0129; 0130; 0150, (2018/04/03)
The invention discloses application of Cu-MOF (Metal Organic Framework) type catalyst in preparing polysubstitution pyridine derivative. The method for carrying out catalytic preparation on the polysubstitution pyridine derivative by the Cu-MOF type catalyst comprises the following steps: carrying out cyclization reaction on an even mixing system which contains the Cu-MOF type catalyst, carbonyl compound, propargylamine and solvent at the temperature of room temperature to 100 DEG C to obtain the polysubstitution pyridine derivative. According to the method, the amination/cyclization/arylatingreaction of the catalyzing carbonylation compound of the Cu-MOF type catalyst and propargylamine can be realized for the first time, and various polysubstitution pyridine derivatives can be obtainedat a high yield. The Cu-MOF type catalyst used by the invention is heterogeneous catalyst which is stable for air and water, environment pollution is reduced, the Cu-MOF type catalyst does not need tobe protected by inert gas, a synthesis method is simple, raw material price is low, and the Cu-MOF type catalyst can be reused. Meanwhile, the Cu-MOF type catalyst has the advantages of low reactiontemperature, high reaction selectivity, high efficiency and wide applicable range of substrate.
Compound as potassium channel modulator
-
Paragraph 0638; 0640; 0641; 0642, (2018/07/30)
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
SUBSTITUTE 1, 6-NAPHTHYRIDINES FOR USE AS SCD INHIBITORS
-
Page/Page column 40-41, (2009/06/27)
The present invention relates to substituted tetrahydronaphthyridine (THN) compounds of the formula (I) and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity.
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element
Haginoya, Noriyasu,Kobayashi, Syozo,Komoriya, Satoshi,Yoshino, Toshiharu,Suzuki, Makoto,Shimada, Takashi,Watanabe, Kengo,Hirokawa, Yumiko,Furugori, Taketoshi,Nagahara, Takayasu
, p. 5167 - 5182 (2007/10/03)
Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N-(6-chloronaphthalen-2-yl) sulfonylpiperazine derivatives incorporating various fused-bicyclic rings containing an aliphatic amine expected to be S4 binding element. Among this series, 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine type 61 displayed orally potent anti-fXa activity and evident prolongation of prothrombin time (PT) with the moderate bioavailability in rats. The X-ray crystal analysis afforded an obvious binding mode that 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine and 6-chloronaphthalene respectively bound to S4 and S1 subsites. In this X-ray study, we discovered a novel intramolecular S-O close contact. Ab initio energy calculations of model compounds deduced that conformers with the most close S-O proximity were most stable. The Mulliken population analysis proposed that this energy profile was caused by both of electrostatic S-O affinity and N-O repulsion. The results of these calculations and X-ray analysis suggested a possibility that the restricted conformation effected the affinity to S4 subsite of fXa.
Sequential amination/annulation/aromatization reaction of carbonyl compounds and propargylamine: A new one-pot approach to functionalized pyridines
Abbiati, Giorgio,Arcadi, Antonio,Bianchi, Gabriele,Di Giuseppe, Sabrina,Marinelli, Fabio,Rossi, Elisabetta
, p. 6959 - 6966 (2007/10/03)
A general one-pot synthesis of pyridines 4a-t from the reaction of dialkyl acyclic/cyclic ketones 1a-i, methyl, aryl/heteroaryl ketones 1m-r, and aldehydes bearing α-hydrogens 1s,t with propargylamine 2 is described. Gold and copper salts are efficient catalysts for the reaction of ketones with 2. The formation of the pyridines 4 is suggested to proceed through the sequential amination of carbonyl compounds followed by regioselective 6-endo-dig cyclization of the N-propargylenamine (N-propargyldienamine) intermediate 3(5) and aromatization reaction. Whereas the preparation of linear polycyclic pyridine 4i can be carried out by reacting cholestan-3-one 1i with 2, the angular polycyclic pyridine 4j has been obtained starting from cholest-5-en-3-one 1j. Selectivity of the reaction of polycyclic dicarbonyls 1k,1 with 2 has also been investigated.
Heterocycylic-substituted quinoline-carboxylic acids
-
, (2008/06/13)
1-Substituted-6-fluoro-7-heterocyclic-1,4-dihydroquino-1-(or dihydronaphthyridin)-4-one carboxylic acids have antibacterial properties. The 7-heterocyclic group is a bicyclic group, one of the rings of which is saturated and the other ring of which is unsaturated.
