Diisopropylethylamine → (2-(Pyrid-4-yl)-1h-benzimidazole-4-carbonyl)-(l)-leucine methyl ester

関与物質

役割	名称	HCID	仕込み量
反応物	Diisopropylethylamine	HCID 81531	—
反応物	O-[(Ethoxycarbonyl)cyanomethylenamino]-N,N,N',N'-tetramethyluronium tetrafluoroborate	HCID 2733286	—
反応物	2-Pyridin-4-yl-3H-benzoimidazole-4-carboxylic acid	HCID 11207170	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	(2-(Pyrid-4-yl)-1h-benzimidazole-4-carbonyl)-(l)-leucine methyl ester	HCID 15480893	—

反応手順

120 mg (0.5 mmol) of 2-(pyrid-4-yl)-1H-benzimidazole-4-carboxylic acid (1d) and 84 mg (0.5 mmol) of H-(L)-leucine methyl ester were dissolved in 5 ml of DMF. 164 mg (0.5 mmol) of TOTU and 0.086 ml of diisopropylethylamine were added and the mixture was stirred at RT for 3 h. The precipitate was filtered off and the filtrate was concentrated. The residue was dissolved in ethyl acetate, the solution was washed with water, and the organic phase was dried using anhydrous sodium sulfate and concentrated. Yield: 180 mg (98%).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06358978B1
出典データセット	uspto-grants-2002_03
ORD ID	ord-184fe2b0b5f24a8d8c53a2db5518b886
出典メモ	uspto-grants-2002_03