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HRID 428461作成日:2026年10月24日

Acetonitrile → 7-[2-(t-Butoxycarbonyl)-8-(methoxyimino)-2,6-diazaspiro[3,4]oct-6-yl]-1-cyclopropyl-5-amino-6,8-difluoro-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid

https://huagongshe.com/ja/reaction/428461

反応式

関与物質

役割名称HCID仕込み量
反応物AcetonitrileHCID 6342—
反応物TriethylamineHCID 8471—
反応物5-Amino-1-cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acidHCID 13910947—
反応物2,6-Diazaspiro[3.4]octane-2-carboxylic acid, 8-(methoxyimino)-, 1,1-dimethylethyl esterHCID 54547656—
溶媒DimethylformamideHCID 6228—
生成物7-[2-(t-Butoxycarbonyl)-8-(methoxyimino)-2,6-diazaspiro[3,4]oct-6-yl]-1-cyclopropyl-5-amino-6,8-difluoro-4-oxo-1,4-dihydro-3-quinolinecarboxylic acidHCID 5434966331.3%

反応手順

750 mg of 1-cyclopropyl-5-amino-6,7,8-trifluoro-4-oxo-1,4-dihydro-3-quinoline-carboxylic acid, 1.05 g of t-butyl 8-(methoxyimino)-2,6-diazaspiro[3,4]octane-2-carboxylate and 4 g of Amberlite® IRA-420 were added to 20 ml of acetonitrile and thereto 2 ml of triethylamine was added by dropping. The mixture was refluxed for 5 days and then 2 ml of dimethylformamide was added thereto. The resulting mixture was stirred for 1 hour and thus precipitated solid was filtered off. The filtrate was concentrated under the reduced pressure and then to the resulting residue 10 ml of acetonitrile was added and stirred for 1 hour. The precipitated solid was filtered and dried to give 420 mg of the titled compound(yield: 30.9%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06313299B1
出典データセットuspto-grants-2001_11
ORD IDord-d7fd68198c9d4954a1470470f7d25f9d
出典メモuspto-grants-2001_11