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HRID 875152作成日:2026年10月25日

Morpholine → tert-butoxycarbonyl-(1S)-1-methyl-2-morpholin-4-yl-2-oxo-1-phenylethylamine

https://huagongshe.com/reaction/875152

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物DiisopropylethylamineHCID 81531—
反応物O-benzotriazol-1-yl-tetramethyluroniumHCID 130500—
反応物(S)-2-(Boc-amino)-2-phenylpropanoic acidHCID 13678038—
溶媒DimethylformamideHCID 6228—
生成物tert-butoxycarbonyl-(1S)-1-methyl-2-morpholin-4-yl-2-oxo-1-phenylethylamineHCID 5744416588%

反応手順

630 mg (2.374 mmol) of N-(tert-butoxycarbonyl)-2-phenyl-D-alanine were dissolved in 20 mL of dry DMF and O-(benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoborate (TBTU, 1.37 g, 4.27 mmol), morpholine (0.412 mL, 4.73 mmol) and diisopropylethylamine (1.63 mL, 9.5 mol) were added. The mixture was stirred at room temperature for 1 hour, then the solvent was removed and the residue dissolved with dichloromethane. The solution was washed with saturated NaHCO3, brine, water and dried over Na2SO4. 700 mg of the title compound were recovered (88% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08981089B2
出典データセットuspto-grants-2015_03
ORD IDord-c2fc58b057564997847ea5cd4f374881
出典メモuspto-grants-2015_03