84200-09-9

Upstream product

• 100-43-6 4-vinylpyridine 
• 75-05-8 acetonitrile 
• 108-89-4 picoline 
• 107-13-1 acrylonitrile 
• 5264-02-8 3-(4-pyridyl)-1-chloropropane 
• 151-50-8 potassium cyanide 
• 143-33-9 sodium cyanide 
• 2629-72-3 4-(3-Hydroxypropyl)pyridine 
• 75-09-2 dichloromethane 
• 102878-73-9 γ-(pyridin-4-yl)butyric acid 
• 71879-58-8 4-(4-pyridyl)butanamide 

Downstream Products

• 5264-15-3 4-(4-pyridinyl)butan-1-ol 
• 189938-86-1 N-(4-Pyridin-4-yl-butyl)-acetamide 
• 102878-73-9 γ-(pyridin-4-yl)butyric acid 

Relevant academic research and scientific papers

Preparation method of piperidine-4-butylamine

The invention provides a preparation method of piperidine-4-butylamine, which comprises the following steps: S1, converting pyridine-4-butyric acid into piperidine-4-butyramide under the condition of ammonia gas; S2, enabling the piperidine-4-butyrylamide to react with pyridine, so as to generate pyridine-4-butyronitrile; S3, carrying out a reduction reaction on the pyridine-4-butyronitrile in an acid environment under the action of a catalyst to generate the piperidine-4-butylamine. According to the preparation method provided by the embodiment of the invention, the reaction steps are short, the safety of raw materials is high, and the experimental operability is very strong.

Nα-Imidazolylalkyl and Pyridylalkyl Derivatives of Histaprodifen: Synthesis and in Vitro Evaluation of Highly Potent Histamine H1-Receptor Agonists

A novel series of Nα-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen (6, 2-[2-(3,3-diphenylpropyl)imidazol-4-yl]ethanamine) was synthesized and evaluated as histamine H1-receptor agonists. The title compounds displayed partial agonism at contractile H1-receptors of guinea pig ileum and were at least equipotent with histamine. Agonist effects of the new derivatives were susceptible to blockade by the H1-receptor antagonist mepyramine (2-100 nM). In the imidazole series, suprahistaprodifen (51, [2-[2-(3,3-diphenylpropyl)-1H-imidazol-4-yl]ethyl]-[2-(1H-imidazol-4-yl) ethyl]amine, Nα-2-[(1H-imidazol-4-yl)ethyl]histaprodifen) showed the highest H1-receptor agonist potency ever reported in the literature (pEC50 8.26, efficacy Emax 96%). Elongation of the alkyl spacer from ethyl to butyl decreased activity from 3630% (ethyl, 51) to 163% (butyl, 53) of histamine potency. The exchange of the terminal imidazole nucleus for a pyridine ring resulted in compounds with comparably high potency. A decrease in agonist potency and efficacy was observed when the attachment of the alkyl spacer was consecutively changed from the ortho to the meta and the para position, respectively, of the pyridine ring. The pyridine series that contained a butyl chain possessed the highest potency and affinity. Nα-[4-(2-pyridyl)butyl]histaprodifen (56) emerged as a strong partial agonist, being almost equipotent with 51 (pEC50 8.16, E max 89%). Compounds 51 and 56 also showed potent partial agonism at contractile H1 receptors in guinea pig aorta and potently activated H1-receptor-mediated endothelium-dependent relaxation in the rat aorta. Compounds 51-65 displayed low to moderate affinity at H2, H3, and M3 receptors in functional models of guinea pig. Collectively, Nα-imidazolylalkyl- and Nα -pyridylalkyl-substituted histaprodifens represent a novel class of potent H1-receptor agonists. These compounds may be useful to define the (patho)physiological role of the H1-receptor and refine molecular models of H1-receptor activation.

Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands

Syntheses of four novel amide analogues of the muscarinic M2 receptor antagonists, DIBA and BIBN 140, are described from a common intermediate. Pharmacological evaluation through in vitro assays reveals high muscarinic receptor affinity in each of the compounds, but variable subtype selectivity, primarily M2 but in one case M3.

Substituted dibenzoxazepine and dibenzthiazepine carbamate compounds, pharmaceutical compositions and methods of use

The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a com

Substituted dibenzoxazepine and dibenzthiazepine urea compounds, pharmaceutical compositions and methods of use

The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a com

HOMOLYTIC CYANOETHYLATION OF ALKYLPYRIDINES

It was shown by the method of competing reactions that the reactivity of alkylpyridines in the homolytic cyanoethylation of 2-, 3-, and 4-picolines and 2-methyl-5-ethylpyridine by acrylonitrile depends on the number and the position of the alkyl groups.All the investigated alkylpyridines are more reactive than toluene in cyanoethylation.

Substituted imidazo[1,5-A]pyridines

Disclosed are e.g. novel 5-(carboxyalkyl)imidazo[1,5-a]pyridines, their derivatives and methods of synthesis. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombo

Certain imidazo (1,5-A) pyridine aliphatic carboxylic acid derivatives and their use as selective thromboxane inhibitors

Disclosed are e.g. 5-(tetrazolylalkyl, hydroxycarbamoylalkyl)imidazo[1,5-a]-pyridines, and methods of synthesis. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thro

Structural Factors Affecting the Basicity of ω-Pyridylalkanols, ω-Pyridylalkanamides and ω-Pyridylalkylamines

The present paper describes the preparation by conventional methods (when not available commercially) and the pKa-determination of the α-, β- and γ-isomers of pyridylethanamide, 3-pyridylpropanamide, 4-pyridylbutanamide, 5-pyridylpentanamide, pyridylmethanol, 2-pyridylethanol, 3-pyridylpropanol, 4-pyridylbutanol, 5-pyridylpentanol, pyridylmethylamine, 2-pyridylethylamine, 3-pyridylpropylamine, 4-pyridylbutylamine, and 5-pyridylpentylamine.While a field effect accounts for many variations in pKa as a function of chain length, marked inductive effects are operative in some methyl and ethyl homologs.The pKa-decreasing influence of an intramolecular H-bond is also apparent in some lower homologs belonging to the α-series.