- Moxifloxacin of a preparation or a pharmaceutically acceptable salt, wherein the method of the midbody
-
The invention provides a novel method for preparing moxifloxacin or its medicinal salt and its intermediate, which comprises the following steps: dissolving boron trioxide in a certain amount of acetic anhydride and an acetate mixing solution, reacting under the temperature of 90-120 DEG C, cooling a reaction solution; adding cyclized quinolinecarboxylic ester in the reaction solution and reacting at the reaction temperature of 50-80 DEG C, cooling, adding a certain amount of an ether solvent, stirring and then filtering, washing by the ether solvent, drying to obtain the product; reacting with (4aR, 7aR)-octahydropyrrolo[3,4-b]pyridine to obtain the moxifloxacin or its medicinal salt. The reaction method of the invention is mild and controllable, the common equipments enable production, the obtained product has the advantages of high purity and good color, boron oxide substitutes boric acid for chelating to reduce the damage of equipments and human body caused by acid mist in the reaction.
- -
-
Paragraph 0037-0038
(2017/03/28)
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF MOXIFLOXACIN HYDROCHLORIDE
-
The present invention relates to an improved process for the preparation of Moxifloxacin hydrochloride from the ethyl 1-cyclopropyl- 6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylate through a novel intermediate (4aS-Cis)-l-cyclopropyl-7-(2,8-diazabicyclo [4.3.0]non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinoline carboxylic acid-03, 04)bis (acyloxy-0) borate.
- -
-
Page/Page column 10-11
(2008/06/13)
-