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HRID 84810作成日:2026年10月26日

Potassium Carbonate → (R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamide

https://huagongshe.com/reaction/84810

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物3-Amino-5-methylisoxazoleHCID 66172—
反応物Binap, (A+-)-HCID 634876—
反応物(R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamideHCID 67509372—
触媒palladium(II) acetateHCID 167845—
溶媒1,4-DioxaneHCID 31275—
生成物(R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamideHCID 6751096419.7%

反応手順

A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide (120 mg, 0.387 mmol), 3-amino-5-methylisoxazole (60 mg, 0.612 mmol), BINAP (40 mg, 0.064 mmol), Pd(OAc)2 (30 mg, 0.13 mmol) and K2CO3 (150 mg, 1.08 mmol) in dioxane (3 mL) was degassed with Ar, then was stirred at 120 C for 18 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamide (25 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846928B2
出典データセットuspto-grants-2014_09
ORD IDord-564a0593e8774134aa927e1dae04c80e
出典メモuspto-grants-2014_09