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HRID 1096236作成日:2026年10月25日

Acetic Acid → 4-[3-(4-Hydroxy-4-phenyl-piperidin-1-yl)-propyl]-1-(3-trifluoromethyl-phenyl)-[1,4]diazepan-5-one

https://huagongshe.com/reaction/1096236

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物4-Phenylpiperidin-4-olHCID 96387—
反応物Borane;pyridineHCID 2723995—
反応物3-[7-Oxo-4-(3-trifluoromethyl-phenyl)-[1,4]diazepan-1-yl]-propionaldehydeHCID 86638388—
溶媒1,2-Dichloroethane ethanolHCID 22901612—
生成物4-[3-(4-Hydroxy-4-phenyl-piperidin-1-yl)-propyl]-1-(3-trifluoromethyl-phenyl)-[1,4]diazepan-5-oneHCID 5915924644%

反応手順

To a solution of 3-[7-oxo-4-(3-trifluoromethyl-phenyl)-[1,4]diazepan-1-yl]-propionaldehyde 0.016 g (0.05 mmol) and 4-phenyl-piperidin-4-ol 0.018 g (0.10 mmol) in DCE/EtOH 1:1 (0.5 ml) was added pyridine-borane complex (25 μL of 8 M solution in pyridine, 0.2 mmol) and AcOH (25 μL, 0.4 mmol) and the mixture stirred for 16 h. The mixture was then evaporated to dryness and purified by preparative HPLC, affording the title compound 0.01 g (44%) as a white solid. MS: 476.2 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08138175B2
出典データセットuspto-grants-2012_03
ORD IDord-08bf37eec1154abcab77aabfd51a5773
出典メモuspto-grants-2012_03