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HRID 1045504作成日:2026年10月26日

Cesium carbonate → 5-[(3-amino-1-methyl-1H-indazol-6-yl)oxy]-3-(4-methoxybenzyl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one

https://huagongshe.com/reaction/1045504

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物5-chloro-3-[(4-methoxyphenyl)methyl]-1H,2H,3H,4H-pyrido[2,3-d]pyrimidin-2-oneHCID 66926291—
反応物3-amino-1-methyl-1H-indazol-6-olHCID 135742460—
溶媒DimethylformamideHCID 6228—
生成物5-[(3-amino-1-methyl-1H-indazol-6-yl)oxy]-3-(4-methoxybenzyl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-oneHCID 7049718570.4%

反応条件

温度130 °C

反応手順

Suspended 5-chloro-3-(4-methoxy-benzyl)-3,4-dihydro-1h-pyrido[2,3-d]pyrimidin-2-one (400.00 mg; 1.32 mmol; 1.00 eq.), 3-amino-1-methyl-1h-indazol-6-ol (268.61 mg; 1.65 mmol; 1.25 eq.) and cesium carbonate (858.15 mg; 2.63 mmol; 2.00 eq.) in DMF (4.00 ml). Heated in a microwave at 130° C. for 90 min. The reaction was concentrated, redissolved in DMSO (20 mL) and filtered through celite. Purified filtrate via prep HPLC to afford 400 mg (56%) of compound 276 as a tan solid. LC-MS (M+H=431, obsd.=431)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08569295B2
出典データセットuspto-grants-2013_10
ORD IDord-ca4ffde5bd114f9091d795fa9afd8acc
出典メモuspto-grants-2013_10