(3-{6-[8-(4-Methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-ylamino}-3-phenyl-propyl)-carbamic acid tert-butyl ester → N1-{6-[8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-yl}-1-phenyl-propane-1,3-diamine

HRID 1186515ノート

反応式

HRID 1186515 の反応式
C(OC(=O)[NH:7][CH2:8][CH2:9][CH:10]([NH:17][C:18]1[CH:23]=[CH:22][CH:21]=[C:20]([C:24]2[N:28]3[CH:29]=[CH:30][N:31]=[C:32]([N:33]4[CH2:38][CH2:37][N:36]([CH3:39])[CH2:35][CH2:34]4)[C:27]3=[N:26][CH:25]=2)[N:19]=1)[C:11]1[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=1)(C)(C)C>C(O)C.Cl>[CH3:39][N:36]1[CH2:35][CH2:34][N:33]([C:32]2[C:27]3[N:28]([C:24]([C:20]4[N:19]=[C:18]([NH:17][CH:10]([C:11]5[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=5)[CH2:9][CH2:8][NH2:7])[CH:23]=[CH:22][CH:21]=4)=[CH:25][N:26]=3)[CH:29]=[CH:30][N:31]=2)[CH2:38][CH2:37]1

参加物

4

反応物 1

HCID 68227060(3-{6-[8-(4-Methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-ylamino}-3-phenyl-propyl)-carbamic acid tert-butyl ester

生成物 1

HCID 66548827N1-{6-[8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-yl}-1-phenyl-propane-1,3-diamine

試薬・触媒・溶媒 2

HCID 313Hydrochloric Acid溶媒HCID 702Ethanol溶媒

実験手順

The solution of (3-{6-[8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-ylamino}-3-phenyl-propyl)-carbamic acid tert-butyl ester (44 mg, 0.08 mmol) in ethanol (4 mL) and concentrated HCl (4 mL) was stirred at room temperature for 15 hours. The reaction mixture was then concentrated under reduced pressure. The residue was suspended in CH2Cl2 and concentrated under reduced pressure to give N1-{6-[8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-yl}-1-phenyl-propane-1,3-diamine; hydrochloride. (Yield 25 mg). 1H NMR (300 MHz, CD3OD): δ 8.39 (s, 1H), 8.15 (s, 1H), 7.61 (t, 1H, J=5.7 Hz), 7.40-7.48 (m, 7H), 6.78 (brs, 1H), 5.39 (brs, 1H), 5.01 (brs, 1H), 3.81-3.66 (m, 4H), 3.37 (brs, 2H), 3.12-2.91 (m, 7H), 2.16-2.14 (m, 2H). LC-MS: [M+H]+ 443.

後処理

  1. concentrationThe reaction mixture was then concentrated under reduced pressure
  2. concentrationconcentrated under reduced pressure

出典と根拠

ORDレコード
ord-70ab128cdfa34787b015181af1fae25f
出典データセット
uspto-grants-2014_03
特許番号
US08673905B2

反応ノート

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