Methanesulfonyl chloride → 4-(benzyloxy)-3-[(1R)-3-(diisopropylamino)-1-phenylpropyl]phenylethyl methanesulfonate

HRID 1433270ノート

反応式

HRID 1433270 の反応式
[CH2:1]([O:8][C:9]1[CH:14]=[CH:13][C:12]([CH2:15][CH2:16][OH:17])=[CH:11][C:10]=1[C@@H:18]([C:28]1[CH:33]=[CH:32][CH:31]=[CH:30][CH:29]=1)[CH2:19][CH2:20][N:21]([CH:25]([CH3:27])[CH3:26])[CH:22]([CH3:24])[CH3:23])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.C(N(CC)C(C)C)(C)C.[CH3:43][S:44](Cl)(=[O:46])=[O:45]>ClCCl>[CH3:43][S:44]([O:17][CH2:16][CH2:15][C:12]1[CH:13]=[CH:14][C:9]([O:8][CH2:1][C:2]2[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=2)=[C:10]([C@@H:18]([C:28]2[CH:29]=[CH:30][CH:31]=[CH:32][CH:33]=2)[CH2:19][CH2:20][N:21]([CH:25]([CH3:26])[CH3:27])[CH:22]([CH3:23])[CH3:24])[CH:11]=1)(=[O:46])=[O:45]

参加物

5

反応条件

温度
0 °C

実験手順

2-{4-(benzyloxy)-3-[(1R)-3-(diisopropylamino)-1-phenylpropyl]phenyl}ethanol (Prepared according to WO1998/43942, 1.0 g, 2.25 mmol) was dissolved in dichloromethane (20 ml) and N,N-diisopropyl ethylamine (1.8 ml, 10 mmol) added. The solution was then cooled to 0° C. and methanesulphonyl chloride (0.42 ml, 5.4 mmol) was added. After stirring for 2 hours at 0° C. the mixture was diluted with dichloromethane (20 ml) and washed with water (50 ml), brine (50 ml) and then dried (magnesium sulphate) and the solvent removed in vacuo to yield the title compound as a yellow oil, 1.56 g.

後処理

  1. washwashed with water (50 ml), brine (50 ml)
  2. dry with materialdried (magnesium sulphate)
  3. customthe solvent removed in vacuo

出典と根拠

ORDレコード
ord-ba437571b2cd44b199e483d24905623a
出典データセット
uspto-grants-2009_11
特許番号
US07612084B2

反応ノート

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