Lithium Hydroxide → 2-Carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid

HRID 575151ノート

反応式

HRID 575151 の反応式
[C:1]([C:4]1[N:5]=[C:6]2[C:12]3[CH:13]=[C:14]([C:18]#[C:19][C:20]([OH:23])([CH3:22])[CH3:21])[C:15]([F:17])=[CH:16][C:11]=3[O:10][CH2:9][CH2:8][N:7]2[C:24]=1[C:25]([O:27]C)=[O:26])(=[O:3])[NH2:2].[Li+].[OH-]>O.C1COCC1>[C:1]([C:4]1[N:5]=[C:6]2[C:12]3[CH:13]=[C:14]([C:18]#[C:19][C:20]([OH:23])([CH3:21])[CH3:22])[C:15]([F:17])=[CH:16][C:11]=3[O:10][CH2:9][CH2:8][N:7]2[C:24]=1[C:25]([OH:27])=[O:26])(=[O:3])[NH2:2]

参加物

4

反応物 2

HCID 3939Lithium HydroxideHCID 86693170Methyl 2-carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylate

生成物 1

HCID 866931712-Carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid

試薬・触媒・溶媒 1

HCID 21881883Oxolane--water (1/1)溶媒

実験手順

Methyl 10-bromo-2-carbamoyl-9-fluoro-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylate (2 g) was reacted with 2-Methyl-3-butyne-ol similar to as described in Procedure E to afford 2 g of methyl 2-carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylate following triteration from water. MS (Q1) 388 (M)+. Methyl 2-carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylate (1.5 g) was saponified with LiOH in water/THF to afford quantitative yield of 2-carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid. MS (Q1) 383 (M)+.

出典と根拠

ORDレコード
ord-bb3a5345db64488a8c63075c5fc54fe0
出典データセット
uspto-grants-2015_05
特許番号
US09034866B2

反応ノート

読み込み中…