- A PROCESS FOR A PREPARATION OF MARBOFLOXACIN AND INTERMEDIATE THEREOF
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The present invention describes a novel process for the preparation of marbof loxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula (III), NR1R2R3R4, wherein R1, R2, R3 and R4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula (II), wherein R is selected from H, alkyl, arylalkyl, alkali metal cation,, NH4 cation, NR1R2R3R4cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.
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Page/Page column 28
(2011/06/19)
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- A process for a preparation of marbofloxacin and intermediate thereof
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The present invention describes a novel process for the preparation of marbofloxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula III, NR1R2R3R4 wherein R1, R2, R3 and R4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula II, wherein R is selected from H, alkyl, arylalkyl, alkali metal cation, , NH4 cation, NR1R2R3R4cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.
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Page/Page column 16
(2011/06/26)
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- Cycloaracylation of Enamines,II. - Synthesis of 1-Amino-4-quinolone-3-carboxylic Acids
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The 2-benzoyl-3-hydrazinoacrylic esters 3, 11, 17, and 23 are obtained by the reactions of 2-chloro-5-nitrobenzoyl chloride (1) with the enehydrazinocarboxylic esters 2 and 2-benzoyl-3-ethoxyacrylic esters 9 with hydrazine derivatives 10, 16, and 22.After cyclocondensation, the above esters afford 1-aminoquinolonecarboxylic esters 4, 12, 18, and 24, which are hydrolyzed to give the corresponding 1-aminoquinolonecarboxylic acids 5, 13, 19, and 26.The 1-amino-7-haloquinolonecarboxylic acids 13a-f, 19a-f, and 26b react with aliphatic amines to afford 1,7-diaminoquinolonecarboxylic acids 30c-m, which possess a high level of bactericidal activity.
- Grohe, Klaus,Heitzer, Helmut
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p. 871 - 880
(2007/10/02)
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