Triethylamine → HCID 131724455、化合物

関与物質

役割	名称	HCID	仕込み量
反応物	Triethylamine	HCID 8471	—
反応物	1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide	HCID 15908	—
反応物	3,4,5-Trimethoxyphenylacetic acid	HCID 70372	—
反応物	1-Hydroxybenzotriazole	HCID 75771	—
反応物	HCID 22713955	HCID 22713955	—
触媒	4-(Dimethylamino)pyridine	HCID 14284	—
溶媒	Dichloromethane	HCID 6344	—
生成物	HCID 131724455	HCID 131724455	66%

反応手順

To a stirred solution of racemic 5-(3-aminocyclopentyl)-9-chloro-3-methyl-5H-isoxazolo[4,3-c]quinolin-4-one (81 mg, 0.26 mmol) in CH2Cl2 (3 mL) was added 3,4,5-trimethoxy phenyl acetic acid (114 mg, 0.52 mmol), Et3N (0.1 mL, 0.50 mmol), HOBt (41 mg, 0.3 mmol),DMAP (catalytic amount) and EDCI (72 mg, 0.38 mmol). The reaction mixture was stirred at r.t. for 18 hours. The mixture was diluted with CH2Cl2, washed (brine), dried (Na2SO4), filtered and concentrated. Column chromatography (silica gel, hexanes/ethyl acetate, gradient) gave the racemic title compound (89 mg, 66%). Mass Spectrum (FIA) (m/z) 454.0 (M+1)

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06743794B2
出典データセット	uspto-grants-2004_06
ORD ID	ord-3f64bbca03c94c9d838d6d8d06135089
出典メモ	uspto-grants-2004_06