Trifluoroacetic acid → 1-(4-Fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid[1-methyl-6-(2-oxo-1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidin-5-yloxy)-1H-indazol-3-yl]-amide

関与物質

役割	名称	HCID	仕込み量
反応物	Trifluoroacetic acid	HCID 6422	—
反応物	1-(4-Fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylicacid{6-[3-(4-methoxy-benzyl)-2-oxo-1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidin-5-yloxy]-1-methyl-1H-indazol-3-yl}-amide	HCID 70497011	—
生成物	1-(4-Fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid[1-methyl-6-(2-oxo-1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidin-5-yloxy)-1H-indazol-3-yl]-amide	HCID 70498209	82.5%

反応条件

温度	80 °C

反応手順

A solution of compound 278 (22.00 mg; 0.03 mmol; 1.00 eq.) and trifluoroacetic acid (2.00 ml) was stirred at 80 degrees C. overnight. The reaction was stirred at 80 degrees C. for 22 hr. The reaction was concentrated, redissolved in DMSO, and treated with Et3N to pH 8. The solution was then purified directly via prep HPLC to afford 13 mg (60%) of 279 as a yellow solid. LC-MS (M+H=526, obsd.=526).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08569295B2
出典データセット	uspto-grants-2013_10
ORD ID	ord-e29d7cace7f14278a10abbbf4ee75ec7
出典メモ	uspto-grants-2013_10