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HRID 332789作成日:2026年10月26日

Potassium Carbonate → (R)-2-(5-cyano-6-(2-oxo-1,2,3,4-tetrahydroquinolin-6-ylamino)pyrazin-2-ylamino)butanamide

https://huagongshe.com/reaction/332789

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Binap, (A+-)-HCID 634876—
反応物6-amino-3,4-dihydroquinolin-2(1H)-oneHCID 4912759—
反応物(R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)butanamideHCID 86685581—
触媒palladium(II) acetateHCID 167845—
溶媒1,4-DioxaneHCID 31275—
生成物(R)-2-(5-cyano-6-(2-oxo-1,2,3,4-tetrahydroquinolin-6-ylamino)pyrazin-2-ylamino)butanamideHCID 8668558659%

反応手順

A mixture of (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)butanamide (80 mg, 0.334 mmol), 6-amino-3,4-dihydroquinolin-2(1H)-one (60 mg, 0.370 mmol), K2CO3 (100 mg, 0.724 mmol), BINAP (25 mg, 0.040 mmol) and Pd(OAc)2 (10 mg, 0.044 mmol) in dioxane (2 mL) was degassed with Ar, then was stirred at 110 C for 4 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(5-cyano-6-(2-oxo-1,2,3,4-tetrahydroquinolin-6-ylamino)pyrazin-2-ylamino)butanamide (72 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08877760B2
出典データセットuspto-grants-2014_11
ORD IDord-77271ab94614443fb5becbfe526e2306
出典メモuspto-grants-2014_11