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HRID 925623作成日:2026年10月27日

Triethylamine → 8-amino-5-bromo-N-[(1S,2S)-2-hydroxycyclohexyl]-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxamide

https://huagongshe.com/reaction/925623

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 151348—
反応物(1S,2S)-2-aminocyclohexanolHCID 7057408—
反応物8-Amino-5-bromo-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxylic acidHCID 89188577—
溶媒DimethylformamideHCID 6228—
生成物8-amino-5-bromo-N-[(1S,2S)-2-hydroxycyclohexyl]-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxamideHCID 89216070—

反応手順

To a solution of 8-amino-5-bromo-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxylic acid (600 mg, 2.10 mmol) in DMF (7 mL) at rt was added (1S,2S)-2-aminocyclohexanol (242 mg, 2.10 mmol), BOP (1.16 g, 2.63 mmol), and Et3N (0.59 mL, 4.21 mmol). The mixture was stirred at rt for 2 h. The resulting solution was quenched with 10% aqueous NaHCO3 and extracted with ethyl acetate. The combined extracts were washed with water and brine, dried (Na2SO4), and concentrated to afford 8-amino-5-bromo-N-[(1S,2S)-2-hydroxycyclohexyl]-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxamide in pure form.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09284312B2
出典データセットuspto-grants-2016_03
ORD IDord-40109f755ad14a5fb00c93bb855a2006
出典メモuspto-grants-2016_03