Lithium Hydroxide → Cyclopropanesulfonic acid [4,5-difluoro-6-(2-fluoro-4-bromo-phenylamino)-2-methyl-benzooxazol-7-yl]-amide

HRID 1914904ノート

反応式

HRID 1914904 の反応式
[Br:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:12]3[C:13]([F:22])=[C:14]([F:21])[C:15]4[N:16]=[C:17]([CH3:20])[O:18][C:19]=4[C:11]=3[N:10]([S:23]([CH:26]3[CH2:28][CH2:27]3)(=[O:25])=[O:24])C2=O)=[C:4]([F:30])[CH:3]=1.[Li+].[OH-].FC1C2N=COC=2C(NS(C2CC2)(=O)=O)=C(NC2C=CC(I)=CC=2F)C=1F>O>[Br:1][C:2]1[CH:7]=[CH:6][C:5]([NH:8][C:12]2[C:13]([F:22])=[C:14]([F:21])[C:15]3[N:16]=[C:17]([CH3:20])[O:18][C:19]=3[C:11]=2[NH:10][S:23]([CH:26]2[CH2:28][CH2:27]2)(=[O:24])=[O:25])=[C:4]([F:30])[CH:3]=1

参加物

5

反応物 3

HCID 3939Lithium HydroxideHCID 53241452Cyclopropanesulfonic acid [4,5-difluoro-6-(2-fluoro-4-iodo-phenylamino)-benzooxazol-7-yl]-amideHCID 672372936-(4-Bromo-2-fluoro-phenyl)-8-cyclopropanesulfonyl-4,5-difluoro-2-methyl-6,8-dihydro-imidazo [4',5':3,4]benzo[1,2-d]oxazol-7-one

生成物 1

HCID 53241562Cyclopropanesulfonic acid [4,5-difluoro-6-(2-fluoro-4-bromo-phenylamino)-2-methyl-benzooxazol-7-yl]-amide

試薬・触媒・溶媒 1

HCID 962Water溶媒

実験手順

Compound 1H was prepared from 6-(4-bromo-2-fluoro-phenyl)-8-cyclopropanesulfonyl-4,5-difluoro-2-methyl-6,8-dihydro-imidazo[4′,5′:3,4]benzo[1,2-d]oxazol-7-one (I-26a: 100 mg, 0.2 mmol) and LiOH (50 mg, 1.25 mmol) in water (2 mL) using procedures analogous to those described above for Compound 1A to afford 30 mg of the product (31.57% yield). H1NMR (CDCl3, 300 MHz): δ 7.30-7.24 (m, 1H), 7.11 (dt, 1H), 6.56 (s, 1H), 6.54-6.46 (m, 1H), 6.33 (s, 1H), 2.70 (s, 3H), 2.68-2.60 (m, 1H), 1.24-1.16 (m, 2H), 1.04-0.96 (m, 2H). LCMS: 95.35%, m/z=474.0 (M-2). HPLC: 93.89%

出典と根拠

ORDレコード
ord-f551a3a104384ff9929b476c81725730
出典データセット
uspto-grants-2013_12
特許番号
US08614239B2

反応ノート

読み込み中…