1,1-Dimethylethyl [(4r)-4-(5-chloro-2-cyano-4-fluorophenoxy)-4-(1-methyl-1h-imidazol-2-yl)butyl]-carbamate → 2-[[(1r)-4-Amino-1-(1-methyl-1h-imidazol-2-yl)butyl]oxy]-4-chloro-5-fluoro-benzonitrile hydrochloride

HRID 352133ノート

反応式

HRID 352133 の反応式
[Cl:1][C:2]1[C:3]([F:29])=[CH:4][C:5]([C:27]#[N:28])=[C:6]([CH:26]=1)[O:7][C@@H:8]([C:20]1[N:21]([CH3:25])[CH:22]=[CH:23][N:24]=1)[CH2:9][CH2:10][CH2:11][NH:12]C(=O)OC(C)(C)C>Cl.O1CCOCC1>[ClH:1].[NH2:12][CH2:11][CH2:10][CH2:9][C@@H:8]([O:7][C:6]1[CH:26]=[C:2]([Cl:1])[C:3]([F:29])=[CH:4][C:5]=1[C:27]#[N:28])[C:20]1[N:21]([CH3:25])[CH:22]=[CH:23][N:24]=1

参加物

4

反応物 1

HCID 914130451,1-Dimethylethyl [(4r)-4-(5-chloro-2-cyano-4-fluorophenoxy)-4-(1-methyl-1h-imidazol-2-yl)butyl]-carbamate

生成物 1

HCID 698293472-[[(1r)-4-Amino-1-(1-methyl-1h-imidazol-2-yl)butyl]oxy]-4-chloro-5-fluoro-benzonitrile hydrochloride収率 157%

試薬・触媒・溶媒 2

HCID 313Hydrochloric Acid溶媒HCID 312751,4-Dioxane溶媒

実験手順

The product of step (c) (0.33 g, 0.78 mmol) was dissolved in 4M hydrochloric acid in dioxan (10 ml) and stirred for 10 minutes. The solvent was removed in vacuo and the solid residue triturated with ethyl acetate. The white solid was filtered off and dried under high vacuum to give the title compound (0.22 g, 70%).

後処理

  1. customThe solvent was removed in vacuo
  2. customthe solid residue triturated with ethyl acetate
  3. filtrationThe white solid was filtered off
  4. customdried under high vacuum

出典と根拠

ORDレコード
ord-0baef9a194c84897ad0469f4d9577267
出典データセット
uspto-grants-2004_06
特許番号
US06743939B2

反応ノート

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