1-Butanol → (S)-2-(4-((2-Amino-4-(2-hydroxybutylamino)-6-methylpyrimidin-5-yl)methyl)phenyl)acetic acid

HRID 1617235

反応式

HRID 1617235 の反応式
[OH-:1].[K+].C([CH2:5][C:6]1[CH:32]=[CH:31][C:9]([CH2:10][C:11]2[C:12]([N:23]3[CH2:27][C@H:26]([CH2:28][CH3:29])[O:25]C3=O)=[N:13][C:14](/[N:18]=C/N(C)C)=[N:15][C:16]=2[CH3:17])=[CH:8][CH:7]=1)#N.[CH2:33]([OH:37])CCC>>[NH2:18][C:14]1[N:13]=[C:12]([NH:23][CH2:27][C@@H:26]([OH:25])[CH2:28][CH3:29])[C:11]([CH2:10][C:9]2[CH:8]=[CH:7][C:6]([CH2:5][C:33]([OH:37])=[O:1])=[CH:32][CH:31]=2)=[C:16]([CH3:17])[N:15]=1

参加物

4

反応物 3

HCID 2631-ButanolHCID 14797Potassium HydroxideHCID 87445299N'-[5-[[4-(cyanomethyl)phenyl]methyl]-4-[(5S)-5-ethyl-2-oxo-1,3-oxazolidin-3-yl]-6-methylpyrimidin-2-yl]-N,N-dimethylmethanimidamide

生成物 1

HCID 68414496(S)-2-(4-((2-Amino-4-(2-hydroxybutylamino)-6-methylpyrimidin-5-yl)methyl)phenyl)acetic acid

反応条件

温度
100 °C

実験手順

Aq. 5M KOH (1 ml) was added to a stirred solution of the product from step (vi) (136 mg) in butan-1-ol (2 mL). The solution was heated at 100° C. for 15 h and the solvent evaporated under reduced pressure. The residue was diluted with MeOH (2 mL) and the pH adjusted to ˜7 using acetic acid. The solution was purified by RPHPLC to give the subtitle compound as a white solid, 55 mg.

後処理

  1. customthe solvent evaporated under reduced pressure
  2. additionThe residue was diluted with MeOH (2 mL)
  3. customThe solution was purified by RPHPLC

出典と根拠

ORDレコード
ord-106272be15604e57b604f2f3281df270
出典データセット
uspto-grants-2014_07
特許番号
US08765939B2

関連ノート

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