161117-83-5Relevant articles and documents
Synthesis method of 8-chloro-1, 7-naphthyridine-3-formaldehyde
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Paragraph 0048-0052, (2020/04/17)
The invention discloses a synthesis method of 8-chloro-1, 7-naphthyridine-3-formaldehyde, which comprises the following synthesis steps: 1) taking a compound I 2-methoxy-3-aminopyridine as an initialraw material, protecting amino to obtain a compound II; 2) reacting the compound II with an hydroformylation reagent under an alkaline condition to obtain a compound III; 3) deprotecting the compoundIII under an acidic condition to obtain a compound IV or a salt of the compound IV; 4) performing cyclization reaction on the compound IV and an acrylate compound under the action of a Lewis acid to prepare a compound V; 5) carrying out chlorination reaction on the compound V and a chlorination reagent to prepare a compound VI; and 6) dissolving the compound VI 8-chloro-1, 7-naphthyridine-3-formate as a raw material in a solvent, and reducing under the action of a reducing reagent to directly obtain 8-chloro-1, 7-naphthyridine-3-formaldehyde, namely a compound VII. The preparation method disclosed by the invention has the characteristics of suitability for industrial production, relatively low cost and simple operation.
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors
Labadie, Sharada,Barrett, Kathy,Blair, Wade S.,Chang, Christine,Deshmukh, Gauri,Eigenbrot, Charles,Gibbons, Paul,Johnson, Adam,Kenny, Jane R.,Kohli, Pawan Bir,Liimatta, Marya,Lupardus, Patrick J.,Shia, Steven,Steffek, Micah,Ubhayakar, Savita,Abbema, Anne Van,Zak, Mark
, p. 5923 - 5930 (2013/10/22)
A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity. The crystal structures of two representative inhibitors bound to Jak1 were obtained to enable SAR exploration.
Preparation of azaindolines and benzoyl substituted azaindolines: Precursors of triazabenzo[cd]azulen-9-one PDE4 inhibitors
Badland, Matthew,Devillers, Ingrid,Durand, Corinne,Fasquelle, Véronique,Gaudillire, Bernard,Jacobelli, Henry,Manage, Ajith C.,Pevet, Isabelle,Puaud, Jocelyne,Shorter, Anthony J.,Wrigglesworth, Roger
supporting information; experimental part, p. 5292 - 5296 (2011/10/30)
The syntheses of various substituted azaindolines are described. Azaindolines were identified as potential key intermediates towards new PDE4 inhibitors.
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists
Mizutani, Takashi,Nagase, Tsuyoshi,Ito, Sayaka,Miyamoto, Yasuhisa,Tanaka, Takeshi,Takenaga, Norihiro,Tokita, Shigeru,Sato, Nagaaki
scheme or table, p. 6041 - 6045 (2009/06/30)
Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H3 receptor inverse agonists. After systematic modification of lead 5a, the potent and selective analog 5r was identified. Elimination of hERG K+ channel and human α1A-adrenoceptor activities is the main focus of the present study.
QUINAZOLINE DERIVATIVE
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Page/Page column 75, (2010/11/25)
This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R 1 represents a lower alkyl group et al; R 2 and R 3 are same and different and represents hydrogen atm et al; R 4 represents the substituent of the formula (II) et al; X 1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
N-phenylamide and N-pyridylamide derivatives, method of preparing them and pharmaceutical compositions containing them
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Page column 13, (2010/01/30)
The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.
Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives
Rewcastle, Gordon W.,Denny, William A.,Winters, R. Thomas,Colbry, Norman L.,Showalter, H. D. Hollis
, p. 2221 - 2226 (2007/10/03)
Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines with BuLi-TMEDA in diethyl ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids. Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones by reaction with formamide or, more optimally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-butyl dicarbonate in the absence of added base.
Method for preparing alkyl-5,11-dihydro-6h-dipyrido[3,2-B:2',3'-E] [1,4] diazepin-6-ones
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, (2008/06/13)
A method for preparing certain 4-alkyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-ones, which employs the following reaction scheme: STR1
A Simple Method for the Protection of Aryl Amines as their t-Butylcarbamoyl (Boc) Derivatives
Kelly, Terence A.,McNeil, Daniel W.
, p. 9003 - 9006 (2007/10/02)
It has been found that aryl amines can be directly protected as their Boc derivatives by treatment of the amine with two equivalents of NaHMDS in THF followed by one equivalent of di-t-butyldicarbonate.This procedure works on a wide variety of both electron-rich and electron-deficient aryl amines.