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HRID 49924作成日:2026年10月26日

Triethylamine → Methyl 2-Acetamido-3-[2-[(2R)-4-benzyloxycarbonyl-2-(t-butoxycarbonylamino)butoxy]-4-cyanophenyl]acrylate

https://huagongshe.com/reaction/49924

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Tri-o-tolylphosphineHCID 80271—
反応物Methyl 2-acetamidoacrylateHCID 98644—
反応物Benzyl (4R)-4-t-butoxycarbonylamino-5-(5-cyano-2-iodophenoxy)pentanoateHCID 86588382—
触媒palladium(II) acetateHCID 167845—
溶媒DimethylformamideHCID 6228—
生成物Methyl 2-Acetamido-3-[2-[(2R)-4-benzyloxycarbonyl-2-(t-butoxycarbonylamino)butoxy]-4-cyanophenyl]acrylateHCID 69143806—

反応手順

5.72 g (10.4 mmol) of benzyl (4R)-4-t-butoxycarbonylamino-5-(5-cyano-2-iodophenoxy)pentanoate was stirred together with 3.0 g (21 mmol) of methyl 2-acetamidoacrylate, 2.0 g (6.6 mmol) of tris(2-methylphenyl)phosphine, 270 mg (1.1 mmol) of palladium (II) acetate and 3.54 g (35 mmol) of triethylamine in 50 ml of DMF at 100° C. for 5 hours. The solvent was evaporated, and the residue was treated with ethyl acetate as the extracting solvent by an ordinary method and then purified by the silica gel chromatography (ethyl acetate/hexane) to obtain the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06710056B2
出典データセットuspto-grants-2004_03
ORD IDord-715fd5431d2c4d67a7b5470583916518
出典メモuspto-grants-2004_03