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

HRID 2104971노트

반응식

HRID 2104971 반응식
[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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 679Dimethyl Sulfoxide용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-04f85076da30401888a17ac344529ea9
출처 데이터셋
uspto-grants-2009_08
특허 번호
US07576098B2

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