2-Fluoro-4-nitrophenol → 2-(5-(1,3-Dioxan-2-yl)-1-methyl-1H-imidazol-2-yl)-7-(2-fluoro-4-nitrophenoxy)thieno[3,2-b]pyridine

関与物質

役割	名称	HCID	仕込み量
反応物	2-Fluoro-4-nitrophenol	HCID 9825	—
反応物	Sodium Bicarbonate	HCID 516892	—
反応物	2-(5-(1,3-Dioxan-2-yl)-1-methyl-1H-imidazol-2-yl)-7-chlorothieno[3,2-b]pyridine	HCID 57919499	—
溶媒	Dichloromethane	HCID 6344	—
溶媒	Diphenyl Ether	HCID 7583	—
生成物	2-(5-(1,3-Dioxan-2-yl)-1-methyl-1H-imidazol-2-yl)-7-(2-fluoro-4-nitrophenoxy)thieno[3,2-b]pyridine	HCID 57919527	31.2%

反応条件

温度	180 °C

反応手順

A mixture of 40 (5.9 g, 17.57 mmol), 2-fluoro-4-nitrophenol (5.52 g, 35.1 mmol) and NaHCO3 (1.346 g, 16.02 mmol) in Ph2O (7 mL) was heated to 180° C. for 4 hours. The reaction mixture was cooled to RT and diluted with DCM, filtered and concentrated. Purification of the residue by column chromatography (eluent EtOAc) afforded 41 (2.5 g, 31% yield) as a yellow solid. MS (m/z): 457.1 (M+H).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08846927B2
出典データセット	uspto-grants-2014_09
ORD ID	ord-e1a7d28874144d41bdc7e97b26018276
出典メモ	uspto-grants-2014_09