Indoline → (2-Chloropyridin-4-yl)-(2,3-dihydroindol-1-yl)-methanone

関与物質

役割	名称	HCID	仕込み量
反応物	Indoline	HCID 10328	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	2-Chloroisonicotinic acid	HCID 236985	—
反応物	O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate	HCID 2733207	—
溶媒	Tetrahydrofuran	HCID 8028	—
溶媒	Ethyl Acetate	HCID 8857	—
生成物	(2-Chloropyridin-4-yl)-(2,3-dihydroindol-1-yl)-methanone	HCID 28376039	—

反応手順

400 μL (3.53 mmol) 2,3-dihydro-1H-indole were added to 500 mg (3.17 mmol) 2-chloroisonicotinic acid, 600 μL (3.49 mmol) DIPEA and 1.10 g (3.43 mmol) TBTU in 20 mL THF. The reaction mixture was stirred overnight, diluted with ethyl acetate and washed with 15% potassium carbonate solution (1×), water (1×) and 1M hydrochloric acid (1×). The organic phase was dried on magnesium sulphate, filtered and evaporated down i. vac. The residue was triturated with diisopropylether and suction filtered. The solid was dried at 40° C. in the circulating air dryer.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08829006B2
出典データセット	uspto-grants-2014_09
ORD ID	ord-f7906a4de1474d21a55b05796cf0e145
出典メモ	uspto-grants-2014_09