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HRID 60902作成日:2026年10月23日

Dimethylbarbituric acid → N-(((2S,3R)-3-Methylpiperidin-2-yl)methyl)-5-(trifluoromethyl)pyridin-2-amine

https://huagongshe.com/ja/reaction/60902

反応式

関与物質

役割名称HCID仕込み量
反応物Dimethylbarbituric acidHCID 69860—
反応物(2S,3R)-Allyl 3-methyl-2-(((5-(trifluoromethyl)pyridin-2-yl)amino)methyl)piperidine-1-carboxylateHCID 89748220—
触媒HCID 178418397HCID 178418397—
溶媒DichloromethaneHCID 6344—
生成物N-(((2S,3R)-3-Methylpiperidin-2-yl)methyl)-5-(trifluoromethyl)pyridin-2-amineHCID 89739447—

反応手順

A mixture of (2S,3R)-allyl 3-methyl-2-(((5-(trifluoromethyl)pyridin-2-yl)amino)methyl)piperidine-1-carboxylate (0.528 g, 1.48 mmol), Pd(PPh3)4 (0.086 g, 0.0074 mmol) and 1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione (0.14 g, 0.89 mmol) in DCM (20 mL) was stirred at rt. When the starting material was consumed as judged by reverse-phase HPLC analysis, the reaction was concentrated in vacuo. The crude residue was taken up in EtOAc, and washed with satd. aq. NaHCO3, brine, dried (MgSO4), and concentrated to obtain the crude which was purified by silica gel (0˜100% DCM/EtOAc) to afford the title compound. ESI-MS (m/z): 274 [M+1]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09440982B2
出典データセットuspto-grants-2016_09
ORD IDord-4075ba61013643928e15f440f765ce6f
出典メモuspto-grants-2016_09