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HRID 1513922作成日:2026年10月26日

Tetrahydrofuran → 7,9-Difluoro-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5H-6-oxa-chrysen-2-ol

https://huagongshe.com/reaction/1513922

反応式

関与物質

役割名称HCID仕込み量
反応物TetrahydrofuranHCID 8028—
反応物Ammonium ChlorideHCID 25517—
反応物Potassium tert-butoxideHCID 23665647—
反応物5-(Hydroxy-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methyl)-6-(2,3,5-trifluoro-phenyl)-naphthalen-2-olHCID 67004819—
生成物7,9-Difluoro-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5H-6-oxa-chrysen-2-olHCID 1178506390%

反応手順

Dissolve 5-{hydroxy-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methyl}-6-(2,3,5-trifluoro-phenyl)-naphthalen-2-ol (4.3 g, 3.0 mmol) in dry THF (85 mL). Add KOtBu (2.4 g, 21.3 mmol) and stir at room temperature for 3 hours. Pour into saturated aqueous ammonium chloride and extract twice with methylene chloride. Dry the organic layer with sodium sulfate, filter and concentrate in vacuo to yield 3.7 g (90%) of the title compound: mass spectrum (ion spray) m/z=488.2 (M+H). The mixture is purified by chiral chromatography (conditions P). The two isomers eluted with retention times of 6.9 and 8.6 minutes.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08217032B2
出典データセットuspto-grants-2012_07
ORD IDord-d9546a1889b84eae819866f34a05caf0
出典メモuspto-grants-2012_07