Diisopropylethylamine → 4-Acetyl-N-[6-(1H-indol-4-yl)-1H-indazol-4-yl]-2-morpholinecarboxamide

関与物質

役割	名称	HCID	仕込み量
反応物	Diisopropylethylamine	HCID 81531	—
反応物	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
反応物	4-Acetylmorpholine-2-carboxylic acid	HCID 20598078	—
反応物	6-(1H-indol-4-yl)-1H-indazol-4-amine	HCID 58268019	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	4-Acetyl-N-[6-(1H-indol-4-yl)-1H-indazol-4-yl]-2-morpholinecarboxamide	HCID 44540311	30.1%

反応手順

To a solution of HATU (0.107 g, 0.28 mmol) in dry DMF (3 ml) was added 4-acetyl-2-morpholinecarboxylic acid (0.05 g, 0.282 mmol). DIPEA (0.098 ml, 0.56 mmol) was added and the mixture was left to stand for 10 min. 6-(1H-indol-4-yl)-1H-indazol-4-amine (0.04 g, 0.14 mmol), dissolved in dry DMF (3 ml) was added and the solution was left to stand at room temperature for 20 hr. DMF was removed by blow down under a stream of nitrogen, then the residue was dissolved and purified by Mass Directed AutoPrep Method B. The solvent was removed in vacuo and product dried in a vacuum oven at 50° C. overnight to give the title compound as a brown oil (17 mg).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08536169B2
出典データセット	uspto-grants-2013_09
ORD ID	ord-9c46e66f17024e1990e7244b6b765a50
出典メモ	uspto-grants-2013_09