- A new cyclobutane ring contraction: The base-induced rearrangement of an a-bromocyclobutanecarboxylic ester
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Contrary to previous reports, reactions of methyl α-bromocyclobutanecaiboxylate 6b with potassium hydroxide or carbonate lead exclusively to 1-(hydroxymethyl)cyclopropanecarboxylic acid 7.
- Estieu, Karine,Ollivier, Jean,Salauen, Jacques
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- 2-(1-bromocyclobutyl) pyridine and synthesis method thereof
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The invention belongs to the technical field of organic synthesis, and relates to 2- (1-bromocyclobutyl) pyridine and a synthesis method thereof. The 2 -(-1bromocyclobutyl) pyridine can be used as a medical intermediate, and the synthetic method of the compound comprises the following steps: by taking tetrahydropyrane- 2-ketone as a raw material, carrying out nine steps of reactions including substitution, ring closing, hydrolysis, substitution, substitution, reduction, grignard, substitution and substitution to prepare the 2- (-1bromocyclobutyl) pyridine, so that the synthetic route is simple, the cost is low, and the efficiency is high.
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- SPIROCYCLIC COMPOUNDS AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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The present invention relates to novel spirocyclic compounds of formulas (1) and (2) which act as modulators of indoleamine 2,3-dioxygenase (ID01) and to the use of said compounds in the prophylaxis and/or treatment of diseases or conditions mediated by indoleamine 2,3-dioxygenase. The invention further relates to pharmaceutical compositions comprising the novel compounds.
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Page/Page column 76
(2019/11/12)
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- MONOBACTAMS
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The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections.
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Page/Page column 124-125
(2012/06/16)
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- (DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES
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The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 40
(2009/10/09)
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- A novel series of parenteral cephalosporins exhibiting potent activities against Pseudomonas aeruginosa and other Gram-negative pathogens: Synthesis and structure-activity relationships
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A series of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(carboxymethoxyimino)acetamido]cephalosporins bearing a 1-(substituted)-1H-pyrrolo[3,2-b]pyridinium group at C-3′ position was synthesized and their in vitro antibacterial activities against Pseudomonas aeruginosa and other Gram-negative pathogens were evaluated. Among the cephalosporins prepared, 7β-[2-(2-amino-5-chlorothiazol-4yl)-2(Z)-((S)-1-carboxyethoxyimino)acetamido]cephalosporins (42d) showed potent antibacterial activities against P. aeruginosa and other Gram-negative pathogens including the strains which produce class C β-lactamase and extended spectrum β-lactamase (ESBL). These results imply that both the Cl atom on the C-7 aminothiazole moiety and the α-substituent at the iminoether moiety are essential for the stability against β-lactamase and the potent activity against Gram-negative bacteria including P. aeruginosa.
- Yamawaki, Kenji,Nomura, Takashi,Yasukata, Tatsuro,Uotani, Koichi,Miwa, Hideaki,Takeda, Kei,Nishitani, Yasuhiro
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p. 6716 - 6732
(2008/03/28)
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- Homolytic aromatic substitution: A radical approach towards the synthesis of 5-azaoxindoles
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A range of 5-azaoxindoles have been synthesised employing homolytic aromatic substitution onto pyridine as the pivotal step.
- Storey, John M.D.,Ladwa, Mitesh M.
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p. 381 - 383
(2007/10/03)
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