1836-62-0Relevant articles and documents
Design and synthesis of new potent 5-HT7 receptor ligands as a candidate for the treatment of central nervous system diseases
Drabczyk, Anna K.,Ja?kowska, Jolanta,Ku?aga, Damian,Latacz, Gniewomir,Pla?uk, Damian,Rózga, Karolina,Sata?a, Grzegorz
supporting information, (2021/10/29)
Owing to their multifunctional pharmacological profiles (including dual 5-HT1A/5-HT7 action), arylpiperazine derivatives are widely used for treating central nervous system diseases including the depression or neuropathic pain. Herein we describe the design, synthesis and evaluation of biological activity of novel 5-HT7 ligands derived of 2,4,6-triamino-1,3,5-triazine. The studied compounds showed affinity and high selectively towards 5-HT7 receptor with the two most active compounds 34 (Ki = 61 nM), 22 (Ki = 109 nM) showing good metabolic stability and moderate affinity to CYP3A4 isoenzyme. Compound 22 had high hepatotoxicity at a concentration below 50 μM, while compound 34 showed low hepatotoxicity even at a concentration above 50 μM.
Synthesis method of 2-(2-methoxyphenoxy)ethylamine
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Paragraph 0026-0034, (2022/01/08)
The invention provides a synthesis method of 2-(2-methoxyphenoxy)ethylamine, and belongs to the technical field of organic synthesis. According to the invention, guaiacol, urea and ethanolamine are taken as starting raw materials, and the 2-(2-methoxyphenoxy)ethylamine is synthesized by completing a three-step reaction through a 'one-pot method'. The invention provides a brand new synthesis thought of 2-(2-methoxyphenoxy)ethylamine, innovatively avoids direct use of expensive 2-oxazolidinone, uses urea and ethanolamine to synthesize 2-oxazolidinone, and then directly reacts with guaiacol under the catalysis of alkali to generate 2-(2-methoxyphenoxy)ethylamine.
Preparation method for 2-(2-methoxyphenoxy)ethylamine
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Paragraph 0017, (2019/01/24)
The invention provides a preparation method for 2-(2-methoxyphenoxy)ethylamine. The preparation method comprises the following steps: synthesizing 2-(2-methoxyphenoxy)ethanol with guaiacol as a starting material; then synthesizing 2-(2-methoxyphenoxy)chloroethane through chlorination; then reacting 2-(2-methoxyphenoxy)chloroethane with potassium phthalimide to obtain N-(o-methoxyphenoxyethyl)-phthalimide; and finally, performing basic hydrolysis to obtain 2-(2-methoxyphenoxy)ethylamine. The yields of the above four steps of reactions are that the yield of 2-(2-methoxyphenoxy)ethanol is 98.9%;the yield of 2-(2-methoxyphenoxy)chloroethane is 93.7%; the yield of N-(o-methoxyphenoxyethyl)-phthalimide is 86.4%; the yield of 2-(2-methoxyphenoxy)ethylamine is 91.2%; and the total yield of the four steps is 73.04%, which is higher than the yield of 43% in conventional production processes. The preparation method of the invention reduces the production cost of 2-(2-methoxyphenoxy)ethylamine and is safe in the production process.