Potassium Carbonate → 2-[4-[2-[(4-Fluorophenyl)methyl-methylamino]ethyl]pyrazol-1-yl]pyridine-4-carbonitrile

関与物質

役割	名称	HCID	仕込み量
反応物	Potassium Carbonate	HCID 11430	—
反応物	1-(4-fluorophenyl)-N-methylmethanamine	HCID 736860	—
反応物	2-[1-(4-Cyanopyridin-2-yl)pyrazol-4-yl]ethyl methanesulfonate	HCID 86725665	—
溶媒	Acetonitrile	HCID 6342	—
生成物	2-[4-[2-[(4-Fluorophenyl)methyl-methylamino]ethyl]pyrazol-1-yl]pyridine-4-carbonitrile	HCID 86725664	50.3%

反応条件

温度	80 °C

反応手順

To a mixture of 2-[1-(4-cyanopyridin-2-yl)pyrazol-4-yl]ethyl methanesulfonate (476 mg, 1.6 mmol) and (4-flouro-benzyl)-methyl-amine (444 mg, 3.2 mmol) in ACN (30 mL) at rt was added K2CO3 (4.5 g, 32 mmol) and KI (1.0 g, 6.2 mmol. The reaction mixture was heated to 80° C. and stirred overnight. Filtered, solvent removed and purified by prep-HPLC to give the title compound (270 mg, 50%). [M+H] Calc'd for C19H18FN5, 336. Found, 336.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09107916B2
出典データセット	uspto-grants-2015_08
ORD ID	ord-86447b2a9d744996b4ac6bc4175d3280
出典メモ	uspto-grants-2015_08