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HRID 902337作成日:2026年10月25日

Methanol → {[(R)-8-(2-methoxyphenyl)-6-fluoro-2H-chromen-2-yl]methyl}amine

https://huagongshe.com/reaction/902337

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物TriphenylphosphineHCID 11776—
反応物(R)-2-azidomethyl-8-(2-methoxyphenyl)-6-fluoro-chromanHCID 86609113—
溶媒WaterHCID 962—
溶媒DichloromethaneHCID 6344—
溶媒TetrahydrofuranHCID 8028—
溶媒Ammonium HydroxideHCID 14923—
生成物{[(R)-8-(2-methoxyphenyl)-6-fluoro-2H-chromen-2-yl]methyl}amineHCID 59701548—

反応手順

To a solution of (R)-2-azidomethyl-8-(2-methoxyphenyl)-6-fluoro-chroman (190 mg, 0.32 mmol) in tetrahydrofuran (10 mL) and water (0.5 mL) was added triphenylphosphine (0.26 g, 10 mmol) and the reaction mixture stirred at room temperature for 24 hours. The solvent was removed under vacuum to form a colorless oil. Chromatography with 0–5% methanol in methylene chloride plus 1% NH4OH afforded {[(R)-8-(2-methoxyphenyl)-6-fluoro-2H-chromen-2-yl]methyl}amine as a colorless oil. The colorless oil was dissolved in ethyl acetate and made into its hydrochloride salt (119 mg, 61%) as an off-white crystalline solid, mp 198–200° C.; [α]D25=+173.89° (c=5.2 mg/0.7mL MeOH).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07365095B2
出典データセットuspto-grants-2008_04
ORD IDord-df21f2ee12534b0d992aa75e82bebba5
出典メモuspto-grants-2008_04