- Preparation of 3 - chloro - 2 - aminomethyl - 5 - trifluoromethyl pyridine (by machine translation)
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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)
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Paragraph 0064; 0065; 0066; 0067; 0068; 0069-0078
(2017/08/24)
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- Preparation method of 2-aminomethyl-3-chloro-trifluoromethyl pyridine
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The invention discloses a preparation method of 2-aminomethyl-3-chloro-trifluoromethyl pyridine. The method includes the following steps that 2-cyano-3-chloro-5-trifluoromethyl pyridine is adopted as a raw material, a polar solvent and alkaline matter are added, the materials react under the heating condition, after the raw materials react completely, reaction liquid is cooled to the low-temperature condition, alkaline matter and hypohalous acid salt are added, after an intermediate product 2-(3-chloro-5-trifluoromethyl-2-pyridine)acetamide reacts completely, part of the solvent is steamed out in a pressure reduction mode, cooling, filtering, washing and vacuum drying are carried out, and 2-aminomethyl-3-chloro-trifluoromethyl pyridine is prepared. The preparation method of 2-aminomethyl-3-chloro-trifluoromethyl pyridine has the following advantages that a high-pressure reaction is avoided, the raw materials are easy to purchase, aftertreatment operation is simple, the yield is high, the product quality is high, and environmental pollution is low.
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Paragraph 0018; 0019
(2017/02/09)
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- CATALYTIC HYDROGENATION OF SUBSTITUTED CYANOPYRIDINES AND PROCESS FOR PREPARING SUBSTITUTED PYRIDYLMETHYLBENZAMIDES
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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.
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Page/Page column 50
(2016/12/16)
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- A process for preparing 2 - aminomethyl - 3 - chloro - 5 - trifluoromethyl pyridine (by machine translation)
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The invention discloses a process for preparing 2 - aminomethyl - 3 - chloro - 5 - trifluoromethyl pyridine. Comprising the following steps: to 2, 3 - dichloro - 5 - trifluoromethyl pyridine as raw materials, phase transfer catalyst is added, the alkaline substance under certain temperature and nitromethane to carry out the reaction of 3 - chloro - 2 - nitro-methyl - 5 - trifluoro methyl pyridine; then in the ionic liquid and is in Ni/SiO2 Catalytic hydrogenation reduction to obtain 2 - aminomethyl - 3 - chloro - 5 - trifluoro methyl pyridine. The invention provides a process for preparing 2 - aminomethyl - 3 - chloro - 5 - trifluoromethyl pyridine has the following advantages: the raw material is easy to buy, simple post treatment operation, the raw material can be recycled, high yield, good product quality and environmental pollution is relatively small and the like. (by machine translation)
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Paragraph 0023; 0026; 0029; 0032; 0035
(2017/05/06)
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- Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
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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.
- Zhang, Yu-Juan,Shen, Liu-Lan,Cheon, Hyae-Gyeong,Xu, Yong-Nan,Jeong, Jin-Hyun
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p. 588 - 599
(2014/06/09)
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- Synthesis of novel imidazo[1,5-a]pyridine derivates
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An new, efficient synthesis of imidazo[1,5-a]pyridine derivatives starting from (3-chloro-5-(trifluoromethyl)pyridine-2- yl)methanamine(1) has been developed. A protocol to a 100 g scale synthesis of the amine (1) is given. Good yields are obtained. The structures of two products were confirmed by single crystal X-ray methods.
- Mihorianu, Monica,Mangalagiu, Ionel,Jones, Peter G.,Daniliuc, Constantin-Gabriel,Franz, M. Heiko,Neda, Ion
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p. 689 - 695
(2011/10/18)
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- Novel process for the preparation of 2-aminomethylpyridine derivative
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Process for the preparation of 2-aminomethylpyridine derivative of general formula (I) or a salt thereof : ???in which :n represents 0, 1, 2 or 3,X is halogen atom,each Y may be the same or different and may be a halogen atom, a halogenoalkyl, an alkoxycarbonyl or an alkylsulphonyl.
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Page column 3
(2008/06/13)
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