1-(1H-Imidazol-1-yl)ethanone → HCID 16747179, 화합물

HRID 20059

반응식

HRID 20059 반응식
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

참가 물질

6

반응물 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

생성물 1

HCID 16747179HCID 16747179, 화합물수율 24.7%

시약·촉매·용매 2

HCID 887Methanol용매HCID 6228Dimethylformamide용매

실험 절차

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.

후처리

  1. custompurified on Shimadzu HPLC

출처 및 근거

ORD 기록
ord-811784750c46412ea16a8463960b8434
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745484B2

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