Methanol → [(4-dipropylamino-butyl)-(4-{[(1-methoxycarbonylmethyl-1H-imidazol-2-ylmethyl)-(1-methyl-1H-imidazol-2-ylmethyl)-amino]-methyl}-benzyl)-amino]-acetic acid methyl ester

HRID 2080840ノート

反応式

HRID 2080840 の反応式
[NH:1]1[CH:5]=[CH:4][N:3]=[C:2]1[CH2:6][N:7]([CH2:15][C:16]1[CH:34]=[CH:33][C:19]([CH2:20][NH:21][CH2:22][CH2:23][CH2:24][CH2:25][N:26]([CH2:30][CH2:31][CH3:32])[CH2:27][CH2:28][CH3:29])=[CH:18][CH:17]=1)[CH2:8][C:9]1[N:10]([CH3:14])[CH:11]=[CH:12][N:13]=1.C(N(CC)CC)C.Br[CH2:43][C:44]([O:46][CH3:47])=[O:45].C[OH:49].C1[CH2:54][O:53][CH2:52][CH2:51]1>>[CH3:47][O:46][C:44](=[O:45])[CH2:43][N:21]([CH2:22][CH2:23][CH2:24][CH2:25][N:26]([CH2:27][CH2:28][CH3:29])[CH2:30][CH2:31][CH3:32])[CH2:20][C:19]1[CH:33]=[CH:34][C:16]([CH2:15][N:7]([CH2:6][C:2]2[N:3]([CH2:51][C:52]([O:53][CH3:54])=[O:49])[CH:4]=[CH:5][N:1]=2)[CH2:8][C:9]2[N:10]([CH3:14])[CH:11]=[CH:12][N:13]=2)=[CH:17][CH:18]=1

参加物

6

反応物 5

HCID 887MethanolHCID 8028TetrahydrofuranHCID 8471TriethylamineHCID 60984Methyl bromoacetateHCID 58801930CXCR4 antagonist 1

生成物 1

HCID 67103883[(4-dipropylamino-butyl)-(4-{[(1-methoxycarbonylmethyl-1H-imidazol-2-ylmethyl)-(1-methyl-1H-imidazol-2-ylmethyl)-amino]-methyl}-benzyl)-amino]-acetic acid methyl ester

実験手順

The compound (81.9 mg) obtained in Example 52-3 was dissolved in THF (2.0 ml) and added with triethylamine (76.0 μl) and methyl bromoacetate (46.0 μl) and the whole was stirred at room temperature for 11 hours under a nitrogen atmosphere. After completion of the reaction, the solution was added with methanol and the solvent was distilled off under reduced pressure. The residue was purified through silica gel column chromatography (chloroform/methanol), thereby obtaining the subject compound (23.7 mg) as a yellow oily substance.

後処理

  1. customAfter completion of the reaction
  2. distillationthe solvent was distilled off under reduced pressure
  3. customThe residue was purified through silica gel column chromatography (chloroform/methanol)

出典と根拠

ORDレコード
ord-711fdf2b5d4e4a9f941fab4121203091
出典データセット
uspto-grants-2011_04
特許番号
US07932281B2

反応ノート

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