Tetrahydrofuran → 2-(6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-pyridin-3-yl)-propan-2-ol

HRID 42208

反応式

HRID 42208 の反応式
C(OC(=O)[C:5]1[CH:10]=[CH:9][C:8]([N:11]2[CH2:16][CH2:15][N:14]([C:17]3[C:26]4[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=4)[C:20]([CH2:27][C:28]4[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=4)=[N:19][N:18]=3)[CH2:13][CH2:12]2)=[N:7][CH:6]=1)C.[CH3:36][Mg]I.[CH2:39]1[CH2:43][O:42]CC1>>[F:34][C:31]1[CH:32]=[CH:33][C:28]([CH2:27][C:20]2[C:21]3[C:26](=[CH:25][CH:24]=[CH:23][CH:22]=3)[C:17]([N:14]3[CH2:13][CH2:12][N:11]([C:8]4[N:7]=[CH:6][C:5]([C:43]([OH:42])([CH3:39])[CH3:36])=[CH:10][CH:9]=4)[CH2:16][CH2:15]3)=[N:18][N:19]=2)=[CH:29][CH:30]=1

参加物

4

反応物 3

HCID 8028TetrahydrofuranHCID 592406536-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid ethyl esterHCID 178418373HCID 178418373、化合物

生成物 1

HCID 592405842-(6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-pyridin-3-yl)-propan-2-ol収率 10%

実験手順

6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid ethyl ester (85 mg, 0.180 mmol) is dissolved in THF (1 mL). Methyl magnesium iodide (240 μL, 3M in diethyl ether, 0.72 mmol) is added dropwise. Stir reaction for 2 h at room temperature. Concentrate in vacuo. The residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2) to afford the title compound (8 mg, 10%).

後処理

  1. customreaction for 2 h at room temperature
  2. concentrationConcentrate in vacuo
  3. customThe residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2)

出典と根拠

ORDレコード
ord-ea976603e2204ac9bd075527618ef6cc
出典データセット
uspto-grants-2013_09
特許番号
US08536168B2

関連ノート

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