Methanesulfonyl chloride → Methanesulfonic acid 2-(4-{2-[2-(3,5-difluoro-phenyl)-acetylamino]-pentanoylamino}-imidazol-1-yl)-ethyl ester

HRID 1714383ノート

反応式

HRID 1714383 の反応式
[OH:1][CH2:2][CH2:3][N:4]1[CH:8]=[C:7]([NH:9][C:10](=[O:27])[CH:11]([NH:15][C:16](=[O:26])[CH2:17][C:18]2[CH:23]=[C:22]([F:24])[CH:21]=[C:20]([F:25])[CH:19]=2)[CH2:12][CH2:13][CH3:14])[N:6]=[CH:5]1.[CH3:28][S:29](Cl)(=[O:31])=[O:30]>N1C=CC=CC=1>[F:25][C:20]1[CH:19]=[C:18]([CH2:17][C:16]([NH:15][CH:11]([CH2:12][CH2:13][CH3:14])[C:10]([NH:9][C:7]2[N:6]=[CH:5][N:4]([CH2:3][CH2:2][O:1][S:29]([CH3:28])(=[O:31])=[O:30])[CH:8]=2)=[O:27])=[O:26])[CH:23]=[C:22]([F:24])[CH:21]=1

参加物

4

反応物 2

HCID 31297Methanesulfonyl chlorideHCID 115960342-[2-(3,5-Difluoro-phenyl)-acetylamino]-pentanoic acid [1-(2-hydroxy-ethyl)-1H-imidazol-4-yl]-amide

生成物 1

HCID 86600814Methanesulfonic acid 2-(4-{2-[2-(3,5-difluoro-phenyl)-acetylamino]-pentanoylamino}-imidazol-1-yl)-ethyl ester

試薬・触媒・溶媒 1

HCID 1049Pyridine溶媒

実験手順

2-[2-(3,5-Difluoro-phenyl)-acetylamino]-pentanoic acid [1-(2-hydroxy-ethyl)-1H-imidazol-4-yl]-amide (1 equiv) was dissolved in pyridine and treated with methansulfonyl chloride (2.2 equiv) at 0° C. The reaction was warmed to rt and stirred for 4 h, quenched with sodium bicarbonate, and extracted with methylene chloride. The extracts were dried and concentrated to provide methanesulfonic acid 2-(4-{2-[2-(3,5-difluoro-phenyl)-acetylamino]-pentanoylamino}-imidazol-1-yl)-ethyl ester which was used without further purification.

後処理

  1. customquenched with sodium bicarbonate
  2. extractionextracted with methylene chloride
  3. customThe extracts were dried
  4. concentrationconcentrated

出典と根拠

ORDレコード
ord-67c50d9056b94f77ae3a5e8877a6d174
出典データセット
uspto-grants-2010_09
特許番号
US07795447B2

反応ノート

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