Triethylamine → 3-(2,5-Difluoro-phenyl)-N-{1-[3-(pyridin-4-ylamino)-phenyl]ethyl}-acrylamide

関与物質

役割	名称	HCID	仕込み量
反応物	Triethylamine	HCID 8471	—
反応物	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
反応物	(S)-[3-(1-amino-ethyl)-phenyl]-pyridin-4-yl-amine	HCID 60004117	—
反応物	2.5-Difluoro-chlorocinnamic acid	HCID 86759747	—
触媒	4-(Dimethylamino)pyridine	HCID 14284	—
溶媒	Dichloromethane	HCID 6344	—
生成物	3-(2,5-Difluoro-phenyl)-N-{1-[3-(pyridin-4-ylamino)-phenyl]ethyl}-acrylamide	HCID 69800304	81.7%

反応手順

A mixture of (S)-[3-(1-amino-ethyl)-phenyl]-pyridin-4-yl-amine (0.1 mmol), 2.5-difluoro-chlorocinnamic acid (0.1 mmol), EDAC.HCl (0.2 mmol), DMAP (0.1 mmol), triethylamine (0.3 mmol) in dichloromethane (2 mL) was stirred at room temperature overnight. The reaction mixture was purified by flash chromatography with 5% methnol in ethyl acetate to provide the title compound (31 mg) as a solid.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06900210B2
出典データセット	uspto-grants-2005_05
ORD ID	ord-516a3a37db3a4d388f037877ad273a50
出典メモ	uspto-grants-2005_05