- Process for preparing N- ethylpyridine methylamine hydrochloride crystal, and application thereof in preparation of itemamide (by machine translation)
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An application N - of,ethylpyridine methylamine hydrochloride crystal, prepared by dissolving N -ethylpyridine methylamine N - in an organic solvent, at room temperature or heating X - in an organic solvent is stirred until the material is completely dissolved, is stirred until the material is completely dissolved or stirred at about 9.73 °, 14.61 °, 17.98 °, 18.49 °, 20.36 °, 24.63 °, 27.21 ° with a diffraction peak, and is stirred. N - through a,ray powder diffractogram, for drying to obtain the supported product amide key starting material, ethyl-pyridine methylamine hydrochloride; is prepared by filtering, and drying. The crystal has the advantages of simple operation, purification effect, crystallization and high N -purity crystal, form impurity content in the, preparation of the itemamide hydrochloride, crystal . and is, simple and convenient, operation. (by machine translation)
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Paragraph 0019-0021
(2020/05/02)
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- N- Ethylpyridine methylamine hydrochloride and crystal, preparation process and application thereof
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The invention discloses N -ethyl-pyridine methylamine trifluoroacetate, and a crystal. preparation process and application N - thereof to prepare N -ethylpyridine methylamine hydrochloride crystals, by slowly adding X -ethyl-pyridine methylamine, in an organic solvent 15.12 °, 15.45 °, 17.68 °, 20.68 °, 22.62 °, 23.25 °, 24.75 °, 29.54 ° at room temperature or heating. to fully dissolve N -ethyl-pyridine methylamine . through heating for, hours to prepare the ethyl-pyridine methylamine trifluoroacetate crystals . The method is simple in operation and;% in crystal form impurity content, obtained by dry-adding trifluoroacetic acid; crystals, at about, at room temperature or, in a heating mode of heating the crystals at a temperature ranging from, N - degrees, to a. material completely-dissolving solution.
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Paragraph 0042-0044
(2020/03/17)
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- N-ethylpyridine methylamine mesylate crystal, preparation process thereof and application of N-ethylpyridine methylamine mesylate crystal in preparation of tropicamide
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The invention discloses an N-ethylpyridine methylamine mesylate crystal, a preparation process thereof and the application of the N-ethylpyridine methylamine mesylate crystal in the preparation of tropicamide. Mesylate of N-ethylpyridine methylamine mesylate crystal is prepared from N-ethylpyridine methylamine and methylsulfonic acid, when X-ray powder diffraction is used, and the crystal has diffraction peaks at about 9.49 degrees, 13.16 degrees, 16.18 degrees, 19.10 degrees, 20.54 degrees, 23.24 degrees, 26.96 degrees and 34.63 degrees. The preparation method comprises the following steps ofdissolving the N-ethylpyridine methylamine in an organic solvent, and stirring at room temperature or heating and stirring until a material is completely dissolved; slowly adding acid, and crystallizing; and carrying out heat preservation aging, filtering and drying to obtain the tropicamide key starting material N-ethylpyridine methylamine mesylate crystal. The method is simple to operate and obvious in purification effect, the salt form impurity content and the crystal form impurity content prepared by crystallization are low, the purity is high, and the industrial production is facilitated.
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Paragraph 0018-0020
(2020/04/17)
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- 2-ARYL IMIDAZO[1,2-A]PYRIDINE-3-ACETAMIDE DERIVATIVES, PREPARATION METHODS AND USE THEREOF
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Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and/or preventing central nervous system disease associated with TSPO functional disorder
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Paragraph 0059
(2013/05/09)
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- 2-Aryl Imidazo[1,2-a]Pyridine-3-Acetamide Derivatives, Preparation Methods and Uses Thereof
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Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and/or preventing central nervous system disease associated with TSPO functional disorder
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Paragraph 0122
(2013/08/15)
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- Synthesis and evaluation of novel carbon-11 labeled oxopurine analogues for positron emission tomography imaging of translocator protein (18 kDa) in peripheral organs
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To develop a PET ligand for imaging TSPO in peripheral organs, we designed three novel oxopurine analogues [11C]3a-c (LogD: 1.81-2.17) by introducing a pyridine ring in place of a benzene ring in the lead compound [11C]2 (LogD: 3.48). The desmethyl precursors 10 for radiosynthesis were synthesized by reacting glycine 7 with picolylamines 4, followed by hydrolysis and by Curtius rearrangement with diphenylphosphoryl azide. Methylation of 10a-c with methyl iodide produced unlabeled compounds 3a-c. The radiosynthesis of [11C]3a-c was performed by reacting 10a-c with [11C]methyl iodide. Compounds 3a-c displayed high or moderate in vitro binding affinities (Ki: 5-40 nM) for TSPO. PET with [ 11C]3a-c in rats showed high uptake in the lung, heart, and kidney, which are organs with high TSPO expression. Metabolite analysis with [ 11C]3a showed that radioactivity in these organs mainly corresponded with unchanged [11C]3a. PET with [11C]3a using a rat model of lung inflammation showed a significant signal in the lipopolysaccharide- treated lung.
- Kumata, Katsushi,Yui, Joji,Hatori, Akiko,Fujinaga, Masayuki,Yanamoto, Kazuhiko,Yamasaki, Tomoteru,Kawamura, Kazunori,Wakizaka, Hidekatsu,Nengaki, Nobuki,Yoshida, Yuichiro,Ogawa, Masanao,Fukumura, Toshimitsu,Zhang, Ming-Rong
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experimental part
p. 6040 - 6049
(2011/10/12)
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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- Contribution to the stability of tropicamide solutions (author's transl)
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The course of the degradation of tropicamide solutions was elucidated. Thus, inter alia, intramolecular elimination of water leads to a compound comparable to apoatropine that the authors designated by atropicamide. Furthermore, methods are described that permit (after thin-layer chromatographic repartition) to detect and to determine quantitatively the active principle in the presence of its degradation products. Tropicamide is stable in aqueous solution; eye-drops prepared from such a solution (Mydrum) are stable for no less than 5 years.
- Pohloudek-Fabini,Martin,Gallasch
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p. 184 - 187
(2007/10/02)
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