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HRID 4180作成日:2026年10月23日

Sodium Iodide → [5-(2-Fluoro-phenyl)-1-methyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-2-ylmethyl]-(3-trifluoromethyl-phenyl)-amine

https://huagongshe.com/ja/reaction/4180

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium IodideHCID 5238—
反応物3-(Trifluoromethyl)anilineHCID 7375—
反応物Potassium CarbonateHCID 11430—
反応物1-methyl-2-chloromethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepineHCID 13485644—
溶媒DimethylformamideHCID 6228—
生成物[5-(2-Fluoro-phenyl)-1-methyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-2-ylmethyl]-(3-trifluoromethyl-phenyl)-amineHCID 19766234—

反応手順

According to the method of Example 5, 1-methyl-2-chloromethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (200 mg, 0.66 mmole) and m-trifluoromethyl aniline (319 mg, 1.97 mmole) were combined in 2 ml of dry N,N-dimethylformamide, and potassium carbonate (273 mg, 1.97 mmole) and sodium iodide (198 mg, 1.32 mmole) were added to this mixture (which was heated at 65° C. for 18 hours). After solvent-removal, partitioning, separation, washing, drying and concentrating, the analytical product was obtained via chromatography on silica gel (ethyl acetate-hexane elution, 3:7 v/v) and was shown to be 96% pure by HPLC.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US04724237
出典データセットuspto-grants-1988_02
ORD IDord-0bc03ba9e5e2470fbc42b20b354ea151
出典メモuspto-grants-1988_02