Water → cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-isopropoxypiperidin-1-yl)-4-(2-methoxyethylcarbamoyl)-1,3-thiazole-5-carboxylic acid

HRID 1425218노트

반응식

HRID 1425218 반응식
[Cl:1][C:2]1[N:3]=[C:4]([C:9]([NH:11][C@H:12]2[CH2:17][CH2:16][N:15]([C:18]3[S:19][C:20]([C:30]([O:32]CC)=[O:31])=[C:21]([C:23](=[O:29])[NH:24][CH2:25][CH2:26][O:27][CH3:28])[N:22]=3)[CH2:14][C@H:13]2[O:35][CH:36]([CH3:38])[CH3:37])=[O:10])[NH:5][C:6]=1[CH2:7][CH3:8].O.[OH-].[Li+].O>O1CCCC1>[Cl:1][C:2]1[N:3]=[C:4]([C:9]([NH:11][C@H:12]2[CH2:17][CH2:16][N:15]([C:18]3[S:19][C:20]([C:30]([OH:32])=[O:31])=[C:21]([C:23](=[O:29])[NH:24][CH2:25][CH2:26][O:27][CH3:28])[N:22]=3)[CH2:14][C@H:13]2[O:35][CH:36]([CH3:37])[CH3:38])=[O:10])[NH:5][C:6]=1[CH2:7][CH3:8]

참가 물질

5

반응물 3

HCID 962WaterHCID 168937Lithium hydroxide, monohydrateHCID 86648690Ethyl cis(+/-)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-isopropoxypiperidin-1-yl)-4-(2-methoxyethylcarbamoyl)-1,3-thiazole-5-carboxylate

생성물 1

HCID 86648691cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-isopropoxypiperidin-1-yl)-4-(2-methoxyethylcarbamoyl)-1,3-thiazole-5-carboxylic acid수율 98%

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

Ethyl cis(±)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-isopropoxypiperidin-1-yl)-4-(2-methoxyethylcarbamoyl)-1,3-thiazole-5-carboxylate obtained in Example (149b) (0.180 g, 0.315 mmol) was dissolved in tetrahydrofuran (5 mL). The solution was subjected to the same operation as in Example (1i) using lithium hydroxide monohydrate (52.9 g, 1.26 mmol) and water (5 mL), to obtain 0.167 g of the title compound as a white solid (98%).

출처 및 근거

ORD 기록
ord-2d0c8b46d4454847a736dec018bf9c1b
출처 데이터셋
uspto-grants-2015_01
특허 번호
US08927588B2

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