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HRID 240596作成日:2026年10月27日

5-Fluoro-2-nitrophenol → (2S,4S)-1-tert-butyl 2-methyl 4-(5-fluoro-2-nitrophenoxy)pyrrolidine-1,2-dicarboxylate

https://huagongshe.com/reaction/240596

反応式

関与物質

役割名称HCID仕込み量
反応物5-Fluoro-2-nitrophenolHCID 9937—
反応物TriphenylphosphineHCID 11776—
反応物(2S,4R)-4-Hydroxypyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl esterHCID 2734883—
反応物Diethyl azodicarboxylateHCID 5462977—
溶媒DichloromethaneHCID 6344—
生成物(2S,4S)-1-tert-butyl 2-methyl 4-(5-fluoro-2-nitrophenoxy)pyrrolidine-1,2-dicarboxylateHCID 58413039—

反応条件

温度0 °C

反応手順

Diethylazodicarboxylate (1.76 ml) was added dropwise to a solution of N-Boc-trans-4-hydroxy-L-proline methyl ester (2.74 g), 5-fluoro-2-nitrophenol (1.47 g) and triphenylphosphine (2.93 g) in dichlormethane under cooling at 0° C. The coolant was removed after 20 min and the reaction mixture was stirred at room temperature over the weekend. The solvent was evaporated and the residue war purified by chromatography to give the desired product.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08648068B2
出典データセットuspto-grants-2014_02
ORD IDord-c3706526ba5e40f2a807010243d86d46
出典メモuspto-grants-2014_02