Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Succinic anhydride | HCID 7922 | — |
| Reactant | 8-Fluorociprofloxacin | HCID 122848 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | Sodium Hydroxide | HCID 14798 | — |
| Solvent | 1,4-Dioxane | HCID 31275 | — |
| Product | HCID 11762141 | HCID 11762141 | 55.7% |
Reaction Steps
3.5 g (0.01 mol) of 1-cyclopropyl-6,8-difluoro7-(piperazin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid are dissolved in a mixture of 0.4 g of sodium hydroxide in 20 ml of water, and a solution of 1 g of succinic anhydride in 10 ml of dioxane, and a solution of 0.4 g of sodium hydroxide in 10 ml of water, are simultaneously added dropwise at 20° C. After standing for 12 hours, the mixture is adjusted to pH 5 with 2N hydrochloric acid, and the precipitate is filtered off under suction, washed with water, heated with methanol, filtered off under suction and dried. 2.5 g of 7-[4-(3-carboxypropionyl)-piperazin-1-yl]-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid having a decomposition temperature of 217°-219° C. are obtained. The following compounds are obtained analogously to Example 21:
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US04952695 |
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| Source dataset | uspto-grants-1990_08 |
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| ORD ID | ord-5b854bab73aa4fbaa014f77ad66e70f1 |
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| Source note | uspto-grants-1990_08 |
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