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HRID 2186656作成日:2026年10月27日

1,2-Dichloroethane → (1S,2S)-2-(5-cyclohexylcarbamoyl)pentanoylamino-3-morpholino-1-phenyl-1-propanol

https://huagongshe.com/reaction/2186656

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DichloroethaneHCID 11—
反応物MethanolHCID 887—
反応物TriethylamineHCID 8471—
反応物(1S,2S)-2-amino-3-morpholino-1-phenyl-1-propanolHCID 10513992—
反応物6-(Cyclohexylamino)-6-oxohexanoic acidHCID 22448403—
溶媒DichloromethaneHCID 6344—
生成物(1S,2S)-2-(5-cyclohexylcarbamoyl)pentanoylamino-3-morpholino-1-phenyl-1-propanolHCID 6982134968%

反応手順

A mixed solvent of methylene chloride:methanol=4:1 (10 ml), 5-cyclohexylcarbamoylpentanoic acid (546.0 mg, 2.4 mmol), triethylamine (620 μl, 4.4 mmol) and EDC (460 mg, 2.4 mmol) were added to (1S,2S)-2-amino-3-morpholino-1-phenyl-1-propanol (472.0 mg, 2.0 mmol), followed by stirring overnight. Methylene chloride (100 ml) was added to the reaction solution. After washed with a saturated sodium hydrogen carbonate solution (50 ml), water (50 ml) and saturated brine (50 ml) successively, the organic layer was dried over sodium sulfate and filtered, and the solvent was evaporated under reduced pressure. The resulting crude product was purified by silica gel column chromatography (chloroform:methanol=10:1) to obtain the title compound (607 mg, yield 68.0%) as colorless oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06407064B2
出典データセットuspto-grants-2002_06
ORD IDord-b54169715d0048df991a09d8ca586ae2
出典メモuspto-grants-2002_06