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Conventional quinolone carboxylic acid-based antibacterial agents are inherently weak in antibacterial activity against Gram-positive bacteria, so it is difficult to say that they have sufficient efficacy as a therapeutic drug against these resistant bacteria
And the increase of Staphylococcus aureus (QRSA) resistant to quinolone carboxylic acid antibacterial agents also makes treatment more difficult
[0007] In Patent Document 1, Patent Document 2, Patent Document 3, etc., the same pyridobenzoxazine carboxylic acid derivatives as the compounds of the present invention are reported as antibacterial agents, but their antibacterial activity against Gram-positive bacteria is weak, and there is no Antibacterial activity against above-mentioned resistant bacteria is documented
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[0027] The following examples illustrate the test examples and preparation methods of the compounds of the present invention in detail.
[0030] Boric acid (12.8 g) and acetic anhydride (63.4 g) were mixed, zinc chloride (236 mg) was added, and the mixture was stirred at room temperature for 0.5 hours. To this mixture was added (3R)-9,10-difluoro-3-fluoromethyl-2,3-dihydro-7-oxo-7H-pyrido[1,2,3-d,e][ 1,4] Ethyl benzoxazine-6-carboxylate (22.6 g), stirred at 60°C for 2.5 hours. The reaction solution was concentrated under reduced pressure, and the residue was dissolved in ethyl acetate (300 mL). The solution was washed with saturated aqueous sodium bicarbonate (2 x 200 mL), then water (100 mL), dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified with a silica gel column (dichloromethane: acetone = 7: 1), and the precipitated yellow amorphous was crystallized with a mixture of acetone-diethyl ether to ob...
reference example 2
[0036] Bis(acetate-O)[(3S)-9,10-difluoro-2,3-dihydro-3-methoxymethyl-7-oxo- 7H-pyrido[1,2,3-d,e][1,4]benzoxazine-6-carboxylate-O 6 ，O 7 ] Synthesis of boron
[0037] first step:
[0038] (3S)-9,10-Difluoro-2,3-dihydro-3-hydroxymethyl-7-oxo-7H-pyrido[1,2,3-d,e][1,4] Ethyl benzoxazine-6-carboxylate (1.30g) was suspended in anhydrous dimethyl sulfoxide (40mL), silver (I) oxide (4.63g) and methylated iodine (1.25mL) were added, and the Stir at room temperature for 21 hours. The insoluble matter in the reaction solution was filtered off, and the filtrate was concentrated under reduced pressure. The residue was purified with a silica gel column (dichloromethane:acetone=5:1) to obtain 740 mg of (3S)-9,10-difluoro-2,3-dihydro-3-methoxymethyl as a white powder -Ethyl 7-oxo-7H-pyrido[1,2,3-d,e][1,4]benzoxazine-6-carboxylate.
[0039] MS (EI) m / z: 339 (M + )
[0040] Elemental analysis value (%): C 16 h 15 f 2 NO 5
[0041] Calculated: C: 56.64, H: 4.46, N: 4.13
[0...
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Abstract
The invention discloses a compound represented in general formula (I), which displays excellent antibacterial activity to gram-positive bacteria, in particular to drug-resistant bacteria such as MRSA, PRSP and VRE, wherein, R1 represents methyl, fluoromethyl, methoxymethyl, ethoxy methyl, hydroxymethyl or methylene; R2 represents the lower alkyl with 1 to 3 hydrogen atom and carbon atom or the ester group of pharmaceutically accepted cation and prodrug; R3 represents hydrogen atom or halogen atom; R4 represents lower alkyl with 1 to 3 hydrogen atom and carbon atom, fluoromethyl, trifluoromethyl or fluorine atom; R5 represents hydrogen atom or fluorine atom.
Description
technical field [0001] The present invention relates to a novel 10-(3-cyclopropylaminomethyl-1-pyrrolidinyl)pyridobenzo that not only exhibits a safe and strong antibacterial effect, but also is effective against drug-resistant bacteria that are difficult for conventional antibacterial agents to exhibit efficacy. Oxazine carboxylic acid derivatives and their salts and hydrates. Background technique [0002] Patent Document 1 Japanese Patent Application Laid-Open No. 57-46986 [0003] Patent Document 2 Japanese Patent Application Laid-Open No. 61-204188 [0004] Patent Document 3 Japanese Patent Application Laid-Open No. 62-155282 [0005] Since the development of norfloxacin, the development of quinolone carboxylic acid-based antibacterial agents called new quinolones has been flourishing all over the world, and they currently occupy an important position as therapeutic drugs for infectious diseases. [0006] In recent years, methicillin-resistant Staphylococcus aureus (M...
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