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HRID 711487作成日:2026年10月26日

Water → (R)-Methyl 6-(1-amino-4-methyl-1-oxopentan-2-ylamino)-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinate

https://huagongshe.com/reaction/711487

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物(R)-2-Amino-4-methylpentanamideHCID 7271815—
反応物methyl 6-chloro-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinateHCID 58317582—
溶媒DimethylacetamideHCID 31374—
生成物(R)-Methyl 6-(1-amino-4-methyl-1-oxopentan-2-ylamino)-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinateHCID 6723747511%

反応条件

温度150 °C

反応手順

A mixture of methyl 6-chloro-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinate (82.9 mg, 0.300 mmol) and (R)-2-amino-4-methylpentanamide (39.0 mg, 0.300 mmol) in DMA (2 mL) was stirred at 150° C. for 12 h. Water was subsequently added and the mixture was extracted with EtOAc. The organic layers were washed with saturated aq NaHCO3, water, and brine, were dried over anhydrous Na2SO4, and filtered. The filtrate was concentrated under reduced pressure. The residue was purified by column chromatography (SiO2, EtOAc) to give the title compound as a yellow oil (11.7 mg, 11%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09181255B2
出典データセットuspto-grants-2015_11
ORD IDord-84301540e6f24f8184dd6d90de1a1b9e
出典メモuspto-grants-2015_11