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HRID 552582作成日:2026年10月26日

Triethylamine → 4-(2-Hydroxy-ethoxy)-phenyl-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone

https://huagongshe.com/reaction/552582

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物(S)-(+)-1-(2-Pyrrolidinylmethyl)pyrrolidineHCID 853152—
反応物PyBOPHCID 2724699—
反応物4-(2-Hydroxyethoxy)benzenecarboxylic acidHCID 4312254—
溶媒DichloromethaneHCID 6344—
生成物4-(2-Hydroxy-ethoxy)-phenyl-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanoneHCID 1196041966.2%

反応手順

4-(2-Hydroxy-ethoxy)-benzoic acid (152 mg, 0.84 mmol), (S)(+)-1-(2-pyrrolidinylmethyl)pyrrolidine (193 mg, 1.25 mmol) and triethylamine (303 mg, 3.0 mmol) are dissolved in dichloromethane (5.0 mL) and benzotriazol-1-yloxytris(pyrrolidino)phosphonium hexafluorophosphate (PyBOP) (786 mg, 1.5 mmol) is added to the mixture. The mixture is stirred at room temperature for 3 days. The reaction mixture is diluted with dichloromethane, washed with brine, dried over Na2SO4, filtered and evaporated. The crude product is purified using silica-gel column chromatography (CH2Cl2:2M NH3 in MeOH=20:1) to give 177 mg (66%) of the title compound. Observed Mass 319.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07951826B2
出典データセットuspto-grants-2011_05
ORD IDord-6607de3a9eb3496199ab018dd70bd4ee
出典メモuspto-grants-2011_05