- (S, S) - 2,8-diazabicyclo [4.3.0] nonane preparation method
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The invention relates to a novel preparation method of (S,S)-2,8-diazabicyclo[4.3.0]. The method comprises the steps that: 2,3-pyridine dicarboxylic acid derivative and amide are subjected to condensation, such that 2,3-pyridine dicarboximide is formed; 2,3-pyridine dicarboximide is subjected to protection and hydrogenation reduction, such that 8-substituted-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane is produced; the product is reduced in a borohydride reduction system, such that 8-substituted-2,8-diazabicyclo[4.3.0]nonane is obtained; the product is subjected to optical-active organic acid resolution, such that 8-site protection group is removed, and the final product is obtained. Or, 2,3-pyridine dicarboximide is directly subjected to hydrogenation reduction, such that 7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane is produced; the product is directly reduced in a borohydride reduction system, such that 2,8-diazabicyclo[4.3.0]nonane is produced; the 2,8-diazabicyclo[4.3.0]nonane is subjected to optical-active organic acid resolution, such that the final product is directly obtained. The method provided by the invention is advantaged in simple reaction route. The raw materials are cheap and easy to obtain. The reaction conditions are mild and easy to control. The method is suitable for industrialized productions.
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Paragraph 0064; 0065
(2017/02/09)
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- Moxifloxacin process for the preparation of intermediates (by machine translation)
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The invention discloses a kind of Moxifloxacin process for the preparation of intermediates, MXC-1 with tetrahydrofurfuroxy pyrrolizinone condensation of the first, longer and acrylamide reaction produce MXC-2, MXC -2 passes through the reduction reaction produce MXC-3, MXC -3 hydrogenation to obtain MXC-4, to obtain a target product last MXC divided; the method step brief, the operation is simple, and is suitable for industrial mass production. (by machine translation)
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- NOVEL COMPOUNDS
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There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
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Page/Page column 143
(2008/12/06)
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- Novel heterocyclic antibacterial compounds
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The invention provides heterocyclic organic compounds that inhibit bacterial DNA polymerase IIIC and type II bacterial topoisomerase. The invention further provides compounds that are useful as intermediates in the synthesis of such heterocyclic organic compounds. Syntheses and uses of such heterocyclic organic molecules are also described.
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- 8-vinyl- and 9-ethinyl-quinolone-carboxylic acids
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The invention relates to new 8-vinyl- and 8-ethinylquinolonecarboxylic acids, process for their preparation, and antibacterial agents and feed additives containing them.
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- 7-(1-PYRROLIDINYL)-3-QUINOLONE-AND-NAPHTHYRIDONECARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS AND FEED ADDITIVES
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7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula in which X1 is halogen, X2 is hydrogen, halogen, amino or other radical, R1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical, R2 is hydrogen, alkyl or a dioxolylmethyl radical, R 3 i s A is N, CH, C-halogen, or the like, or forms a bridge with R1, and addition products thereof
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