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HRID 68580作成日:2026年10月23日

Trifluoroacetic acid → C-{2-methyl-5-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-furan-3-yl}-methylamine

https://huagongshe.com/ja/reaction/68580

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物Sodium HydroxideHCID 14798—
反応物{2-Methyl-5-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-furan-3-ylmethyl}-carbamic acid tert-butyl esterHCID 86706654—
溶媒DichloromethaneHCID 6344—
生成物C-{2-methyl-5-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-furan-3-yl}-methylamineHCID 8670665598.7%

反応手順

Trifluoroacetic acid (6.0 ml) is added to a solution of {2-methyl-5-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-furan-3-ylmethyl}-carbamic acid tert-butyl ester (2.05 g) in dichloromethane (20 ml). After 45 min at room temperature, an aqueous solution of NaOH (2M) is added until pH 12 is reached and the reaction mixture is extracted three times with dichloromethane. The combined organic phases are washed with a saturated solution of NaCl, dried over Na2SO4 and concentrated in vacuo to yield C-{2-methyl-5-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-furan-3-yl}-methylamine (1.64 g, compound 2.5 in Table 2) as a light yellow foam. The crude product obtained is used without further purification. MS (HPLC/MS): 410 (MH), Retention time: 1.27 min.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822466B2
出典データセットuspto-grants-2014_09
ORD IDord-a3d259fbdfa2492fa1f1c34f1efc80a0
出典メモuspto-grants-2014_09