Hydroxylamine → 4-((4-bromo-1-trityl-1H-imidazol-2-yl)(5-ethoxy-2-fluoro-3-isopropoxyphenyl)methylamino)-N'-hydroxybenzamidine

HRID 2104971Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2104971
[Br:1][C:2]1[N:3]=[C:4]([N:26]([CH2:35][C:36]2[CH:41]=[C:40]([O:42][CH2:43][CH3:44])[CH:39]=[C:38]([O:45][CH:46]([CH3:48])[CH3:47])[C:37]=2[F:49])[C:27]2[CH:34]=[CH:33][C:30]([C:31]#[N:32])=[CH:29][CH:28]=2)[N:5]([C:7]([C:20]2[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=2)([C:14]2[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=2)[C:8]2[CH:13]=[CH:12][CH:11]=[CH:10][CH:9]=2)[CH:6]=1.[OH2:50].[NH2:51]O>CS(C)=O>[Br:1][C:2]1[N:3]=[C:4]([N:26]([CH2:35][C:36]2[CH:41]=[C:40]([O:42][CH2:43][CH3:44])[CH:39]=[C:38]([O:45][CH:46]([CH3:48])[CH3:47])[C:37]=2[F:49])[C:27]2[CH:28]=[CH:29][C:30]([C:31]([NH2:51])=[N:32][OH:50])=[CH:33][CH:34]=2)[N:5]([C:7]([C:8]2[CH:13]=[CH:12][CH:11]=[CH:10][CH:9]=2)([C:20]2[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=2)[C:14]2[CH:15]=[CH:16][CH:17]=[CH:18][CH:19]=2)[CH:6]=1

Komponenten

5

Edukt 3

HCID 787HydroxylamineHCID 962WaterHCID 688128174-((4-bromo-1-trityl-1H-imidazol-2-yl)(5-ethoxy-2-fluoro-3-isopropoxyphenyl)methylamino)benzonitrile

Produkt 1

HCID 866079354-((4-bromo-1-trityl-1H-imidazol-2-yl)(5-ethoxy-2-fluoro-3-isopropoxyphenyl)methylamino)-N'-hydroxybenzamidine

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 679Dimethyl SulfoxideLösungsmittel

Versuchsvorschrift

To a solution of Intermediate 28.1 (2.00 g, 2.8 mmol) in 3M NH2OH in DMSO (6 mL) (prepared according to example 1) was heated at 60° C. for 3 h. The reaction mixture was poured into water and the resultant precipitate was collected by filtration and dried in vacuo to afford Intermediate 66.1, which was used in the following step without purification.

Aufarbeitung

  1. filtrationthe resultant precipitate was collected by filtration
  2. customdried in vacuo

Quellen und Nachweise

ORD-Eintrag
ord-04f85076da30401888a17ac344529ea9
Quelldatensatz
uspto-grants-2009_08
Patentnummer
US07576098B2

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