Lithium Hydroxide → cis(+/-)-2-(4-{[(4-Bromo-5-methyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid

反応式

[Br:1][C:2]1[N:3]=[C:4]([C:8]([NH:10][C@H:11]2[CH2:16][CH2:15][N:14]([C:17]3[S:18][C:19]([C:23]([O:25]CC)=[O:24])=[C:20]([CH3:22])[N:21]=3)[CH2:13][C@H:12]2[O:28][CH3:29])=[O:9])[NH:5][C:6]=1[CH3:7].[OH-].[Li+]>>[Br:1][C:2]1[N:3]=[C:4]([C:8]([NH:10][C@H:11]2[CH2:16][CH2:15][N:14]([C:17]3[S:18][C:19]([C:23]([OH:25])=[O:24])=[C:20]([CH3:22])[N:21]=3)[CH2:13][C@H:12]2[O:28][CH3:29])=[O:9])[NH:5][C:6]=1[CH3:7]

参加物

反応物 2

HCID 3939Lithium Hydroxide

HCID 86648476ethyl cis(+/-)-2-(4-{[(4-bromo-5-methyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate

生成物 1

HCID 86648475cis(+/-)-2-(4-{[(4-Bromo-5-methyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid収率 61.5%

実験手順

The same operation as in Example (1i) was performed using ethyl cis(±)-2-(4-{[(4-bromo-5-methyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate obtained in Example (31d) (0.19 g, 0.39 mmol) and 2 N lithium hydroxide (4 mL), to obtain 0.11 g of the title compound as a white solid (61%).

出典と根拠

ORDレコード: ord-17984344362c4a81a4f67a44893fa093
出典データセット: uspto-grants-2015_01
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08927588B2

反応ノート

読み込み中…