796845-50-6Relevant academic research and scientific papers
Preparation method of 2-(4-bromo-1-methyl-1H-pyrazol-5-yl)ethanamine
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Paragraph 0019; 0025; 0033, (2017/08/30)
The invention relates to a preparation method of 2-(4-bromo-1-methyl-1H-pyrazol-5-yl)ethanamine. The method comprises the following steps: reacting 1-methylpyrazole used as a raw material to obtain 1-methyl-1H-pyrazole-5-carbaldehyde; adding piperidine and pyridine to obtain a solid 3-(1-methyl-1H-pyrazole-5-yl) acrylic acid; further, adding palladium on carbon into a methanol solution, and introducing hydrogen to obtain 3-(1-methyl-1H-pyrazol-5-yl) propionic acid; furthermore, reacting under roles of bromine and saturated sodium sulphite solution, and performing spinning drying to obtain a solid 3-(4-bromo-1-methyl-1H-pyrazol-5-yl) propionic acid; adding thionyl chloride, tetrahydrofuran, and stronger ammonia water, reacting, dissolving out methyl alcohol, purifying silica gel, eluting ethyl acetate in sequence to obtain 3-(4-bromo-1-methyl-1H-pyrazol-5-yl) propanamide; finally adding NaOH and bromine, and performing ice-bath to obtain 2-(4-bromo-1-methyl-1H-pyrazol-5-yl)ethanamine. The method has the advantages of being clear in steps, little in waste, high in yield, easy to operate and capable of saving raw materials.
Structural requirements for the stability of novel cephalosporins to AmpC β-lactamase based on 3D-structure
Murano, Kenji,Yamanaka, Toshio,Toda, Ayako,Ohki, Hidenori,Okuda, Shinya,Kawabata, Kohji,Hatano, Kazuo,Takeda, Shinobu,Akamatsu, Hisashi,Itoh, Kenji,Misumi, Keiji,Inoue, Satoshi,Takagi, Tatsuya
, p. 2261 - 2275 (2008/12/20)
AmpC β-lactamase is one of the leading causes of Pseudomonas aeruginosa (P. aeruginosa) resistance to cephalosporins. FR259647 is a cephalosporin having a novel pyrazolium substituent at the 3-position and exhibits excellent activity (MIC = 1 μg/mL) again
CEPHEM COMPOUNDS
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Page 22, (2010/02/09)
The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl which may have suitable substituent(s), R2 is amino, protected amino or guanidino, R3 is carboxy or protected carboxy, R4 /sup
