2-Aminopropanol → Ethyl 2-((3R,4S)-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-4-[(2-hydroxy-1-methylethyl)carbamoyl]-1,3-thiazole-5-carboxylate

참여 물질

역할	이름	HCID	투입량
반응물	2-Aminopropanol	HCID 5126	—
반응물	1-Hydroxybenzotriazole	HCID 75771	—
반응물	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
반응물	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	—
생성물	Ethyl 2-((3R,4S)-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-ethoxypiperidin-1-yl)-4-[(2-hydroxy-1-methylethyl)carbamoyl]-1,3-thiazole-5-carboxylate	HCID 67548691	65%

반응 단계

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) (200 mg, 0.40 mmol), 2-amino-1-propanol (0.06 mL, 0.80 mmol), WSC hydrochloride (230 mg, 1.20 mmol) and 1-hydroxybenzotriazole (54 mg, 0.40 mmol), to obtain 144 mg of the title compound as a white solid (65%).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08536197B2
출처 데이터셋	uspto-grants-2013_09
ORD ID	ord-b7a888416be443349d28b350b745604c
출처 메모	uspto-grants-2013_09