100848-70-2Relevant articles and documents
Electrophilic aromatic substitution on pyridine rings. Intramolecular cyclization using N-acyliminium ions
Brodney, Michael A.,Padwa, Albert
, p. 6153 - 6156 (1997)
The reaction of N-acyliminium ions with several activated pyridines resulted in an intramolecular cyclization to provide novel heterocycles. The reaction exhibited a regiochemical preference for cyclization para to the electron donating substitutent.
Palladium-Catalyzed Methylation of Aryl, Heteroaryl, and Vinyl Boronate Esters
Haydl, Alexander M.,Hartwig, John F.
supporting information, p. 1337 - 1341 (2019/02/26)
A method for the direct methylation of aryl, heteroaryl, and vinyl boronate esters is reported, involving the reaction of iodomethane with aryl-, heteroaryl-, and vinylboronate esters catalyzed by palladium and PtBu2Me. This transformation occurs with a remarkably broad scope and is suitable for late-stage derivatization of biologically active compounds via the boronate esters. The unique capabilities of this method are demonstrated by combining carbon-boron bond-forming reactions with palladium-catalyzed methylation in a tandem transformation.
THIAZOLOPYRIMIDINE COMPOUNDS
-
Page/Page column 54, (2012/10/08)
The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
BACTERICIDE COMPOSITION AND METHOD OF CONTROLLING PLANT DISEASE
-
Page/Page column 21, (2008/06/13)
It is to provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing as active ingredients (a) a benzoylpyridine derivative represented by the formula (I) or its salt: (wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2' is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2" is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2' and R2" may form a condensed ring containing an oxygen atom) and (b) at least one another fungicide.
LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, AND METHODS OF MAKING AND USING THEM
-
Page 72, (2010/02/10)
One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues
Wei, Zhi-Liang,Petukhov, Pavel A.,Xiao, Yingxian,Tückmantel, Werner,George, Clifford,Kellar, Kenneth J.,Kozikowski, Alan P.
, p. 921 - 924 (2007/10/03)
Conformationally constrained epibatidine analogues 20a,b and 23a,b were synthesized using a radical cyclization as the key step. Radioligand displacement assays to six defined rat nicotinic acetylcholine receptor (nAChR) subtypes showed that 20a,b bind with moderate affinities, while 23a,b have low affinities. 20a exhibits higher affinity for the β2 containing subtype than for the β4 containing counterpart, while 20b possesses reversed selectivity. Modeling studies suggest that the spatial distribution of the ligand's atoms around the pharmacophore elements may control their nAChR subtype selectivity.
Synthesis of 2-Substituted 4-Pyridylpropionates. Part 2. Alkylation Approach
Adger, Brian M.,Ayrey, Peter,Bannister, Robin,Forth, Michael A.,Hajikarimian, Yousef,et al.
, p. 2791 - 2796 (2007/10/02)
A synthesis of methyl 3-(2-methoxy-4-pyridyl)propionate (2), a key intermediate in the synthesis of the potent long-acting histamine H2-receptor antagonist SK&F 93574 (1), is described.The key step in the synthesis of compound (1) involves alkylation of 2-methoxy-4-methylpyridine (5) with sodium chloroacetate in the presence of sodamide.The scope and limitations of the alkylation is investigated using a variety of electrophiles.The application of this reaction to other 2-substituted 4-methylpyridines is also discussed.