175277-74-4Relevant articles and documents
Preparation of 3 - chloro - 2 - aminomethyl - 5 - trifluoromethyl pyridine (by machine translation)
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Paragraph 0064; 0065; 0066; 0067; 0068; 0069-0078, (2017/08/24)
The present invention provides a process for preparing 3 - chloro - 2 - aminomethyl - 5 - trifluoromethyl pyridine, comprises the following steps: (a) the formula (I) compound glycine ethyl ester hydrochloride in an organic solvent with benzophenone in the reaction, formula (II) compound two benzylidene glycine ethyl ester; (b) the compound of the formula (II) with a compound of formula (III) 2, 3 - dichloro - 5 - trifluoro methyl pyridine in an organic solvent in the reaction, compound of formula (IV); (c) the compound of the formula (IV) with hydrochloric acid in 20 - 25 °C react under the, formula (V) compound; (d) the formula (V) compound with hydrochloric acid in the 90 - 110 °C occur under the reaction, compound of formula (VI) 3 - chloro - 2 - aminomethyl - 5 - trifluoro methyl pyridine; method of the present invention the raw material is cheap, the reaction process is green, solvent and benzophenone can be recovery, low cost and high yield, it is very suitable for industrial production; (by machine translation)
CATALYTIC HYDROGENATION OF SUBSTITUTED CYANOPYRIDINES AND PROCESS FOR PREPARING SUBSTITUTED PYRIDYLMETHYLBENZAMIDES
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Page/Page column 50, (2016/12/16)
The present invention relates to novel processes for the preparation of substituted pyridyl- methylbenzamide derivatives of formula (I), in particular 2,6-dichloro-N- {[3-chloro-5-(trifluoromethyl)- 2-pyridyl]methyl}benzamide (Fluopicolide), and for the catalytic hydrogenation of substituted cyanopyridine derivatives, in particular 3-chloro-2-cyano-5-trifluoromethylpyridine [= Py-CN] to the corresponding substituted 2-methylaminopyridine derivatives, in particular 2-aminomethyl-3-chloro-5- trifluoromethylpyridine [= Py-methylamine] or salts thereof in the presence of metal catalysts such as in particular palladium catalysts, catalytic modifiers and acids.
Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
Zhang, Yu-Juan,Shen, Liu-Lan,Cheon, Hyae-Gyeong,Xu, Yong-Nan,Jeong, Jin-Hyun
, p. 588 - 599 (2014/06/09)
In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of the presence of various functional groups and suitable for parallel operations to enable the rapid generation of libraries of diverse and structurally complex small molecules. Of the compounds synthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a] pyridin-2-yl)phenyl methanesulfonate (8e) was the most potent agonist with an EC50 of 7.89 μM, and thus is the compound with the greatest potential for application. These findings represent a valuable starting point for the design and discovery of small-molecule GLP-1R agonists that can be administered orally.