36404-88-3Relevant academic research and scientific papers
Synthesis of a 1,8-napththyridin-5-one derivative via an intramolecular 1,3-dipolar cycloaddition reaction
Read,Ray
, p. 1595 - 1597 (1995)
Synthesis of a 1,8-naphthyridin-5-one derivative [(5,6,7,8-tetrahydro-(3-chloro-6-hydroxymethyl-8-methyl)-1,8-naphthyri din-5-one (9)] is described starting from 2-chloronicotinic acid using an intramolecular 1,3-dipolar cycloaddition reaction as the key step.
Method for preparing aldehyde and acid by electrochemical dehydrochlorination of polychloromethylpyridine derivatives
-
Paragraph 0035-0037; 0057-0064, (2020/08/27)
The invention discloses a method for preparing aldehyde and an acid by electrochemical dechlorination of a polychloromethylpyridine derivative, the method comprises the following steps: dissolving thepolychloromethylpyridine derivative in an acetic acid and acetate- containing buffer solution to obtain an electrolytic reaction solution; taking the electrolytic reaction solution as a cathode liquid, performing electrolytic reduction dechlorination reaction at a cathode, and hydrolyzing in the solution to obtain a polychlorinated pyridylaldehyde or acid derivative. The polychloromethylpyridinederivative is shown in formula (I), and the product polychlorinated pyridylaldehyde or acid derivative is shown in formula (II): in the formula (I), m is 0, 1, 2, 3 or 4, n is 0 or 1, and R' is an easy-to-oxidize or easy-to-hydrolyze substituent. The m and the R' in the formula (II) are same as that in the formula (I), R is H or OH, no waste acid is generated in the preparation process, the easy-to-oxidize or easy-to-hydrolyze substituent contained in the polychloromethylpyridine derivative and carbon-chlorine bonds on pyridine rings are not affected, and the recovery conversion rate is high.
FUSED BICYLIC PYRIDINE COMPOUNDS AND THEIR USE AS AMPA RECEPTOR MODULATORS
-
Paragraph 0363, (2018/05/03)
Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
A 2 - chloro - 3 - pyridine formaldehyde synthetic method (by machine translation)
-
Paragraph 0028; 0034; 0035; 0036; 0037; 0044; 0045-0047, (2018/01/12)
The invention discloses a 2 - chloro - 3 - pyridyl aldehyde synthesis method, the method to 2 - chloro - 3 - methyl pyridine as raw materials, passes through chlorine chlorinated, ester hydrolysis, oxidation three-step to obtain 2 - chloro - 3 - pyridine formaldehyde product. The method of the invention mild reaction conditions, high yield, low cost, product purity up to 98% or more, and has a good industrial application prospect. (by machine translation)
PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
-
Page/Page column 51, (2016/07/05)
Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists
Hansen, Martin,Jacobsen, Stine Engesgaard,Plunkett, Shane,Liebscher, Gudrun Eckhard,McCorvy, John D.,Br?uner-Osborne, Hans,Kristensen, Jesper Langgaard
supporting information, p. 3933 - 3937 (2015/01/30)
N-Benzyl substitution of phenethylamine 5-HT2A receptor agonists has dramatic effects on binding affinity, receptor selectivity and agonist activity. In this paper we examine how affinity for the 5-HT2A/2C receptors are influenced by N-benzyl substitution of 4-bromo-2,5-dimethoxyphenethylamine derivatives. Special attention is given to the 2′ and 3′-position of the N-benzyl as such compounds are known to be very potent. We found that substitutions in these positions are generally well tolerated. The 2′-position was further examined using a range of substituents to probe the hydrogen bonding requirements for optimal affinity and selectivity, and it was found that small changes in the ligands in this area had a profound effect on their affinities. Furthermore, two ligands that lack a 2′-benzyl substituent were also found to have high affinity contradicting previous held notions. Several high-affinity ligands were identified and assayed for functional activity at the 5-HT2A and 5-HT2C receptor, and they were generally found to be less efficacious agonists than previously reported N-benzyl phenethylamines.
Novel aromatic fluoroolefins via fluoro-Julia-Kocienski olefination
Allendoerfer, Nadine,Es-Sayed, Mazen,Nieger, Martin,Braese, Stefan
scheme or table, p. 3439 - 3448 (2010/12/19)
Fluoroolefins, which play an increasingly important role as peptide mimics in pharmaceuticals and as crop protection agents, are generated using a fluoro-Julia-Kocienski olefination. Their preparation can easily be accomplished using a Mitsunobu reaction and subsequent oxidation to generate the required benzothiazolyl sulfones. The key step of this process was the electrophilic -fluorination of the sulfone with N-fluorobenzenesulfonimide. The last stage of the successful synthesis of the fluoroolefins was the modified Julia-Kocienski olefination under basic conditions. Further functionalization was followed with the application of a Suzuki reaction. Georg Thieme Verlag Stuttgart.
Efficient route to medium-ring benzo- and azabenzo-lactones
Metay, Estelle,Leonel, Eric,Nedelec, Jean-Yves
, p. 889 - 904 (2008/09/17)
The synthesis of precursors of medium-ring benzo- and azabenzo-lactones is performed efficiently from simple ortho-halo aryl and heteroaryl aldehydes. Copyright Taylor & Francis Group, LLC.
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K + channel
Yoshizumi, Takashi,Takahashi, Hirobumi,Miyazoe, Hiroshi,Sugimoto, Yuichi,Tsujita, Tomohiro,Kato, Tetsuya,Ito, Hirokatsu,Kawamoto, Hiroshi,Hirayama, Mioko,Ichikawa, Daisuke,Azuma-Kanoh, Tomoko,Ozaki, Satoshi,Shibata, Yoshihiro,Tani, Takeshi,Chiba, Masato,Ishii, Yasuyuki,Okuda, Shoki,Tadano, Kiyoshi,Fukuroda, Takahiro,Okamoto, Osamu,Ohta, Hisashi
supporting information; experimental part, p. 4021 - 4029 (2009/05/26)
A series of compounds based on 7-{[4-(2-methylphenyl)piperidin-1-yl]methyl} -6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine-9-ol ((-)-8b), a potent and selective opioid receptor-like 1 (ORL1) antagonist, was prepared and evaluated using structure-activity relationship studies with the aim of removing its affinity to human ether-a-go-go related gene (hERG) K+ channel. From these studies, 101 was identified as an optimized structure with respect to ORL1 antagonist activity, and affinity to the hERG K+channel. Furthermore, 101 showed good in vivo antagonism with a wide therapeutic index in regards to adverse cardiovascular effects.
Method of Treating Pathological Blushing
-
Page/Page column 16, (2010/11/29)
A method of treating pathological blushing is disclosed wherein the patient is administered a DP receptor antagonist. Compositions containing DP antagonists are also included.
