Tetrahydrofuran → (S)-N-{1-[4-(2'-Fluoro-3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-phenyl]-ethyl}-acetamide

関与物質

役割	名称	HCID	仕込み量
反応物	Tetrahydrofuran	HCID 8028	—
反応物	Triethylamine	HCID 8471	—
反応物	2,4-Difluoropyridine	HCID 2762838	—
反応物	(S)-N-[1-(piperidin-4-yl-phenyl)-ethyl]-acetamide	HCID 67125510	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	(S)-N-{1-[4-(2'-Fluoro-3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-phenyl]-ethyl}-acetamide	HCID 67125408	—

反応条件

温度	0 °C

反応手順

To 1.41 g (5.74 mmol) (S)-N-[1-(piperidin-4-yl-phenyl)-ethyl]-acetamide (V.1) in 10 mL THF and 10 mL DMF is added 0.80 mL (5.74 mmol) triethylamine and 0.60 g (5.21 mmol) 2,4-difluoropyridine. The mixture is stirred for 12 h at 0° C. Subsequently the mixture is concentrated in vacuo and the residue is purified by HPLC (C18 RP Sunfire; water (+0.1% TFA)/MeOH) to yield the desired product.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09006450B2
出典データセット	uspto-grants-2015_04
ORD ID	ord-9412e83cb8a04cb4b8320fe8a5343f11
出典メモ	uspto-grants-2015_04