Ethanamine, 2-fluoro-, hydrochloride → Ethyl cis(+/-)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-4-[(2-fluoroethyl)carbamoyl]-1,3-thiazole-5-carboxylate

関与物質

役割	名称	HCID	仕込み量
反応物	Ethanamine, 2-fluoro-, hydrochloride	HCID 9995	—
反応物	1-Hydroxybenzotriazole	HCID 75771	—
反応物	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
反応物	cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-5-(ethoxycarbonyl)-1,3-thiazole-4-carboxylic acid	HCID 86648529	—
生成物	Ethyl cis(+/-)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-4-[(2-fluoroethyl)carbamoyl]-1,3-thiazole-5-carboxylate	HCID 86648837	79.3%

反応手順

The same operation as in Example (247a) was performed using cis(±)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-5-(ethoxycarbonyl)-1,3-thiazole-4-carboxylic acid obtained in Example (50a) (250 mg, 0.50 mmol), 2-fluoroethylamine hydrochloride (100 mg, 1.00 mmol), WSC hydrochloride (288 mg, 1.50 mmol) and 1-hydroxybenzotriazole (68 mg, 0.50 mmol), to obtain 216 mg of the title compound as a white solid (79%).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08536197B2
出典データセット	uspto-grants-2013_09
ORD ID	ord-c9b059309a2d4e6792860b6e36a7ff67
出典メモ	uspto-grants-2013_09