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HRID 12134作成日:2026年10月25日

Sodium borohydride → {4-[2-(Aminomethyl)phenyl]phenyl}-n-{2-[n-(5-chloro(2-pyridyl))carbamoyl]-phenyl}carboxamide

https://huagongshe.com/reaction/12134

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium borohydrideHCID 4311764—
反応物N-{2-[N-(5-chloro(2-pyridyl))carbamoyl]phenyl}[4-(2-cyanophenyl)phenyl)carboxamideHCID 22596431—
触媒Cobalt(II) chlorideHCID 24288—
溶媒DimethylformamideHCID 6228—
生成物{4-[2-(Aminomethyl)phenyl]phenyl}-n-{2-[n-(5-chloro(2-pyridyl))carbamoyl]-phenyl}carboxamideHCID 1872771743.1%

反応手順

A mixture of N-{2-[N-(5-chloro(2-pyridyl))carbamoyl]phenyl}[4-(2-cyanophenyl)phenyl]carboxamide (200 mg, 0.442 mmol, 1.0 equiv.), cobalt chloride (86 mg, 0.664 mmol, 1.5 equiv.) and sodium borohydride (50 mg, 1.33 mmol, 3.0 equiv.) in DMF (15 mL) was stirred at 0° C. to rt for 3 days. The reaction was quenched with ice cubes, diluted with DCM (100 mL) and filtered through celite. The filtrate was washed with saturated aqueous NaHCO3. The organic layer was dried over MgSO4, filtered, evaporated and HPLC (C18 reversed phase) eluting with 0.1% TFA in H2O/CH3CN gave {4-[2-(aminomethyl)phenyl]phenyl)-N-(2-[N-(5-chloro(2-pyridyl))carbamoyl]phenyl}carboxamide (87 mg, 43%). MS found for C26H21ClN4O2 (M+H)+: 457.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07727982B2
出典データセットuspto-grants-2010_06
ORD IDord-df56acc56a7b43ff82539f9c599b7997
出典メモuspto-grants-2010_06