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HRID 355993作成日:2026年10月23日

Triethylamine → 5-methoxy-3-[N-(3-(4-fluoro-phenyl)-3-oxo-propyl)-1,2,5,6-tetrahydro-pyridin-3-ylmethyl]-1H-indole

https://huagongshe.com/ja/reaction/355993

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物2-Chloro-4'-fluoropropiophenoneHCID 67672—
反応物5-methoxy-3-(1,2,5,6-tetrahydro-pyridin-3-ylmethyl)-1H-indoleHCID 18940817—
溶媒Diethyl EtherHCID 3283—
溶媒DichloromethaneHCID 6344—
生成物5-methoxy-3-[N-(3-(4-fluoro-phenyl)-3-oxo-propyl)-1,2,5,6-tetrahydro-pyridin-3-ylmethyl]-1H-indoleHCID 18940881—

反応手順

Triethylamine (0.9 ml; 0.0063 mol) was added to a solution of 3-chloro-4'-fluoropropiophenone (1.2 g; 0.0063 mol) in diethyl ether (10 ml). The resulting mixture was stirred for 3 hours at room temperature. Then the mixture was filtered and the filtrate was concentrated under vacuum. The residue was taken up with a mixture of compound of Description 5 [5-methoxy-3-(1,2,5,6-tetrahydro-pyridin-3-ylmethyl)-1H-indole] (0.79 g; 0.0028 mol), triethylamine (0.8 ml; 0.0057 mol) in methylene chloride (20 ml). The reaction mixture was refluxed for 4 hours. Then the reaction was concentrated under vacuum and the residue was triturated with 1N hydrochloric acid. The aqueous phase was decanted, and the guming solid was twice washed with water and triturated with diethyl ether. The title compound hydrochloride was collected by filtration, washed with diethyl ether and recrystallized with a mixture (1/2) of ethyl acetate/acetone. 0.86 g of the desired compound were obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05834493
出典データセットuspto-grants-1998_11
ORD IDord-5ea039a5f66049a6a1bef76935a1c5c5
出典メモuspto-grants-1998_11