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HRID 16356作成日:2026年10月25日

Methanol → tert-butyl [(1R,2R)-2-hydroxy-1-(3,4,5-trifluorophenyl)propyl]carbamate

https://huagongshe.com/reaction/16356

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物TetrahydrofuranHCID 8028—
反応物Potassium CarbonateHCID 11430—
反応物[(1R,2R)-2-tert-butoxycarbonylamino-1-methyl-2-(3,4,5-trifluorophenyl)ethyl]4-nitrobenzoateHCID 68911294—
溶媒WaterHCID 962—
溶媒Ethyl AcetateHCID 8857—
生成物tert-butyl [(1R,2R)-2-hydroxy-1-(3,4,5-trifluorophenyl)propyl]carbamateHCID 6871798695.1%

反応手順

A potassium carbonate powder (6.43 g) was added to a solution mixture of methanol (90 mL) and THF (10 mL) of 4-nitrobenzoic acid (1R,2R)-2-tert-butoxycarbonylamino-1-methyl-2-(3,4,5-trifluorophenyl)ethyl ester (7.03 g). The resulting reaction solution was stirred at room temperature for 1 hr, and ethyl acetate and water were added thereto. The organic layer was separated, washed with saturated saline twice, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. To the obtained residue, diethylether was added. The insoluble matter was removed by filtration, and the filtrate was concentrated. The residue was purified by silica gel column chromatography (toluene:ethyl acetate=6:1) to give 4.49 g of the title compound. The physical property values of this compound were as follows:

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07737141B2
出典データセットuspto-grants-2010_06
ORD IDord-a8f4e62a5cd14e3b94a24f41ed5e48fb
出典メモuspto-grants-2010_06