1-(1H-Imidazol-1-yl)ethanone → HCID 16747179、化合物

HRID 20059

反応式

HRID 20059 の反応式
Cl.Cl.[NH2:3][C@@H:4]([CH2:25][C:26]1[CH:31]=[CH:30][CH:29]=[CH:28][CH:27]=1)[C@H:5]([OH:24])[CH2:6][NH:7][C@@H:8]1[C:17]2[C:12](=[CH:13][CH:14]=[C:15]([Br:18])[CH:16]=2)[O:11][C:10]([CH3:23])([C:19]([F:22])([F:21])[F:20])[CH2:9]1.N1([C:37](=[O:39])[CH3:38])C=CN=C1.CCN(C(C)C)C(C)C>CN(C=O)C.CO>[Br:18][C:15]1[CH:16]=[C:17]2[C:12](=[CH:13][CH:14]=1)[O:11][C@:10]([CH3:23])([C:19]([F:22])([F:21])[F:20])[CH2:9][C@@H:8]2[NH:7][CH2:6][C@@H:5]([OH:24])[C@@H:4]([NH:3][C:37](=[O:39])[CH3:38])[CH2:25][C:26]1[CH:27]=[CH:28][CH:29]=[CH:30][CH:31]=1

参加物

6

反応物 3

HCID 171741-(1H-Imidazol-1-yl)ethanoneHCID 81531DiisopropylethylamineHCID 86614141(2R,3S)-3-amino-1-((4S)-6-bromo-2-methyl-2-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-ylamino)-4-phenylbutan-2-ol dihydrochloride

生成物 1

HCID 16747179HCID 16747179、化合物収率 24.7%

試薬・触媒・溶媒 2

HCID 887Methanol溶媒HCID 6228Dimethylformamide溶媒

実験手順

To a solution of (2R,3S)-3-amino-1-((4S)-6-bromo-2-methyl-2-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-ylamino)-4-phenylbutan-2-ol dihydrochloride (160 mg, 338 mmol) in DMF was added 1-(1H-imidazol-1-yl)ethanone (37.2 mg, 338 μmol) followed by DIPEA (177 μl, 1014 μmol). The reaction was stirred at RT for 30 min, then diluted with MeOH and purified on Shimadzu HPLC to afford 43.0 mg of the title compounds as a mixture. MS m/z: 515, 517.

後処理

  1. custompurified on Shimadzu HPLC

出典と根拠

ORDレコード
ord-811784750c46412ea16a8463960b8434
出典データセット
uspto-grants-2010_06
特許番号
US07745484B2

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