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 43743ノート

反応式

HRID 43743 の反応式
[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]

参加物

5

反応物 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

生成物 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 acid収率 98%

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

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%).

出典と根拠

ORDレコード
ord-18e2b2f33a5b4065865207ea81490be3
出典データセット
uspto-grants-2013_09
特許番号
US08536197B2

反応ノート

読み込み中…